A patent review of anticancer glucocorticoid receptor modulators (2014-present)

References

• De Bosscher K, Haegeman G. Minireview: latest perspectives on antiinflammatory actions of glucocorticoids. Mol Endocrinol. 2009;23:281–291.
   PubMed Web of Science ®Google Scholar
• McMaster A, Ray DW. Drug insight: selective agonists and antagonists of the glucocorticoid receptor. Nat Clin Pract Endocrinol Metab. 2008;4:91–101.
   PubMedGoogle Scholar
• Rhen T, Cidlowski JA. Antiinflammatory action of glucocorticoids–new mechanisms for old drugs. N Engl J Med. 2005;353:1711–1723.
   PubMed Web of Science ®Google Scholar
• Pufall MA. Glucocorticoids and Cancer. Adv Exp Med Biol. 2015;872:315–333.
   PubMed Web of Science ®Google Scholar
• Inaba H, Pui CH. Glucocorticoid use in acute lymphoblastic leukaemia. Lancet Oncol. 2010;11:1096–1106.
   PubMed Web of Science ®Google Scholar
• Pui CH, Evans WE. Treatment of acute lymphoblastic leukemia. N Engl J Med. 2006;354:166–178.
   PubMed Web of Science ®Google Scholar
• Smolej L. The role of high-dose corticosteroids in the treatment of chronic lymphocytic leukemia. Expert Opin Investig Drugs. 2012;21:1009–1017.
   PubMed Web of Science ®Google Scholar
• Kassi E, Moutsatsou P. Glucocorticoid receptor signaling and prostate cancer. Cancer Lett. 2011;302:1–10.
   PubMed Web of Science ®Google Scholar
• Yemelyanov A, Czwornog J, Chebotaev D, et al. Tumor suppressor activity of glucocorticoid receptor in the prostate. Oncogene. 2007;26:1885–1896.
   PubMed Web of Science ®Google Scholar
• Moutsatsou P, Papavassiliou AG. The glucocorticoid receptor signalling in breast cancer. J Cell Mol Med. 2008;12:145–163.
   PubMed Web of Science ®Google Scholar
• Herr I, Pfitzenmaier J. Glucocorticoid use in prostate cancer and other solid tumours: implications for effectiveness of cytotoxic treatment and metastases. Lancet Oncol. 2006;7:425–430.
   PubMed Web of Science ®Google Scholar
• Zhang C, Beckermann B, Kallifatidis G, et al. Corticosteroids induce chemotherapy resistance in the majority of tumour cells from bone, brain, breast, cervix, melanoma and neuroblastoma. Int J Oncol. 2006;29:1295–1301.
   PubMed Web of Science ®Google Scholar
• Sundahl N, Bridelance J, Libert C, et al. Selective glucocorticoid receptor modulation: new directions with non-steroidal scaffolds. Pharmacol Ther. 2015;152:28–41.
   PubMed Web of Science ®Google Scholar
• De Bosscher K, Beck IM, Ratman D, et al. Activation of the glucocorticoid receptor in acute inflammation: the SEDIGRAM concept. Trends Pharmacol Sci. 2016;37:4–16.
   PubMed Web of Science ®Google Scholar
• Burris TP, Solt LA, Wang Y, et al. Nuclear receptors and their selective pharmacologic modulators. Pharmacol Rev. 2013;65:710–778.
   PubMed Web of Science ®Google Scholar
• Sundahl N, Clarisse D, Bracke M, et al. Selective glucocorticoid receptor-activating adjuvant therapy in cancer treatments. Oncoscience. 2016;3:188–202.
   PubMedGoogle Scholar
• Becker DE. Basic and clinical pharmacology of glucocorticosteroids. Anesth Prog. 2013;60:25–31. quiz 32.
   PubMedGoogle Scholar
• Buchwald P, Bodor N. Soft glucocorticoid design: structural elements and physicochemical parameters determining receptor-binding affinity. Pharmazie. 2004;59:396–404.
   PubMed Web of Science ®Google Scholar
• Vandevyver S, Dejager L, Libert C. Comprehensive overview of the structure and regulation of the glucocorticoid receptor. Endocr Rev. 2014;35:671–693.
   PubMed Web of Science ®Google Scholar
• Vegiopoulos A, Herzig S. Glucocorticoids, metabolism and metabolic diseases. Mol Cell Endocrinol. 2007;275:43–61.
   PubMed Web of Science ®Google Scholar
• Hawkins UA, Gomez-Sanchez EP, Gomez-Sanchez CM, et al. The ubiquitous mineralocorticoid receptor: clinical implications. Curr Hypertens Rep. 2012;14:573–580.
   PubMed Web of Science ®Google Scholar
• Cruz-Topete D, Cidlowski JA. One hormone, two actions: anti- and pro-inflammatory effects of glucocorticoids. Neuroimmunomodulation. 2015;22:20–32.
   PubMed Web of Science ®Google Scholar
• Donatti TL, Koch VH, Takayama L, et al. Effects of glucocorticoids on growth and bone mineralization. J Pediatr (Rio J). 2011;87:4–12.
   PubMed Web of Science ®Google Scholar
• Nussinovitch U, de Carvalho JF, Pereira RM, et al. Glucocorticoids and the cardiovascular system: state of the art. Curr Pharm Des. 2010;16:3574–3585.
   PubMed Web of Science ®Google Scholar
• Whirledge S, Cidlowski JA. Glucocorticoids and reproduction: traffic control on the road to reproduction. Trends Endocrinol Metab. 2017;28:399–415.
   PubMed Web of Science ®Google Scholar
• Sapolsky RM, Romero LM, Munck AU. How do glucocorticoids influence stress responses? Integrating permissive, suppressive, stimulatory, and preparative actions. Endocr Rev. 2000;21:55–89.
   PubMed Web of Science ®Google Scholar
• Gensler LS. Glucocorticoids: complications to anticipate and prevent. Neurohospitalist. 2013;3:92–97.
   PubMedGoogle Scholar
• Beato M, Herrlich P, Schutz G. Steroid hormone receptors: many actors in search of a plot. Cell. 1995;83:851–857.
   PubMed Web of Science ®Google Scholar
• Davies P, Rushmere NK. The structure and function of steroid receptors. Sci Prog. 1988;72:563–578.
   PubMed Web of Science ®Google Scholar
• De Iudicibus S, Franca R, Martelossi S, et al. Molecular mechanism of glucocorticoid resistance in inflammatory bowel disease. World J Gastroenterol. 2011;17:1095–1108.
   PubMed Web of Science ®Google Scholar
• Galigniana MD, Echeverria PC, Erlejman AG, et al. Role of molecular chaperones and TPR-domain proteins in the cytoplasmic transport of steroid receptors and their passage through the nuclear pore. Nucleus. 2010;1:299–308.
   PubMed Web of Science ®Google Scholar
• Riggs DL, Roberts PJ, Chirillo SC, et al. The Hsp90-binding peptidylprolyl isomerase FKBP52 potentiates glucocorticoid signaling in vivo. Embo J. 2003;22:1158–1167.
   PubMed Web of Science ®Google Scholar
• Freedman ND, Yamamoto KR. Importin 7 and importin alpha/importin beta are nuclear import receptors for the glucocorticoid receptor. Mol Biol Cell. 2004;15:2276–2286.
   PubMed Web of Science ®Google Scholar
• Echeverria PC, Mazaira G, Erlejman A, et al. Nuclear import of the glucocorticoid receptor-hsp90 complex through the nuclear pore complex is mediated by its interaction with Nup62 and importin beta. Mol Cell Biol. 2009;29:4788–4797.
   PubMed Web of Science ®Google Scholar
• Oakley RH, Sar M, Cidlowski JA. The human glucocorticoid receptor beta isoform. Expression, biochemical properties, and putative function. J Biol Chem. 1996;271:9550–9559.
   PubMed Web of Science ®Google Scholar
• Oakley RH, Jewell CM, Yudt MR, et al. The dominant negative activity of the human glucocorticoid receptor beta isoform. Specificity and mechanisms of action. J Biol Chem. 1999;274:27857–27866.
   PubMed Web of Science ®Google Scholar
• Escriva H, Delaunay F, Laudet V. Ligand binding and nuclear receptor evolution. Bioessays. 2000;22:717–727.
   PubMed Web of Science ®Google Scholar
• Schiller BJ, Chodankar R, Watson LC, et al. Glucocorticoid receptor binds half sites as a monomer and regulates specific target genes. Genome Biol. 2014;15:418.
   PubMed Web of Science ®Google Scholar
• Lim HW, Uhlenhaut NH, Rauch A, et al. Genomic redistribution of GR monomers and dimers mediates transcriptional response to exogenous glucocorticoid in vivo. Genome Res. 2015;25:836–844.
   PubMed Web of Science ®Google Scholar
• Di Silvestre A, Lucafo M, De Iudicibus S, et al. Glucocorticoid receptor interacting co-regulators: putative candidates for future drug targeting therapy. Mini Rev Med Chem. 2017;17:657–666.
   PubMed Web of Science ®Google Scholar
• Presman DM, Hager GL. More than meets the dimer: what is the quaternary structure of the glucocorticoid receptor? Transcription. 2017;8:32–39.
   PubMed Web of Science ®Google Scholar
• Presman DM, Ganguly S, Schiltz RL, et al. DNA binding triggers tetramerization of the glucocorticoid receptor in live cells. Proc Natl Acad Sci USA. 2016;113:8236–8241.
   PubMed Web of Science ®Google Scholar
• Hudson WH, Youn C, Ortlund EA. The structural basis of direct glucocorticoid-mediated transrepression. Nat Struct Mol Biol. 2013;20:53–58.
   PubMed Web of Science ®Google Scholar
• Surjit M, Ganti KP, Mukherji A, et al. Widespread negative response elements mediate direct repression by agonist-liganded glucocorticoid receptor. Cell. 2011;145:224–241.
   PubMed Web of Science ®Google Scholar
• Rao NA, McCalman MT, Moulos P, et al. Coactivation of GR and NFKB alters the repertoire of their binding sites and target genes. Genome Res. 2011;21:1404–1416.
   PubMed Web of Science ®Google Scholar
• Bhandare R, Damera G, Banerjee A, et al. Glucocorticoid receptor interacting protein-1 restores glucocorticoid responsiveness in steroid-resistant airway structural cells. Am J Respir Cell Mol Biol. 2010;42:9–15.
   PubMed Web of Science ®Google Scholar
• Scheinman RI, Gualberto A, Jewell CM, et al. Characterization of mechanisms involved in transrepression of NF-kappa B by activated glucocorticoid receptors. Mol Cell Biol. 1995;15:943–953.
   PubMed Web of Science ®Google Scholar
• Buttgereit F, Scheffold A. Rapid glucocorticoid effects on immune cells. Steroids. 2002;67:529–534.
   PubMed Web of Science ®Google Scholar
• Strehl C, Gaber T, Lowenberg M, et al. Origin and functional activity of the membrane-bound glucocorticoid receptor. Arthritis Rheum. 2011;63:3779–3788.
   PubMedGoogle Scholar
• Mitre-Aguilar IB, Cabrera-Quintero AJ, Zentella-Dehesa A. Genomic and non-genomic effects of glucocorticoids: implications for breast cancer. Int J Clin Exp Pathol. 2015;8:1–10.
   PubMed Web of Science ®Google Scholar
• Scheller K, Sekeris CE, Krohne G, et al. Localization of glucocorticoid hormone receptors in mitochondria of human cells. Eur J Cell Biol. 2000;79:299–307.
   PubMed Web of Science ®Google Scholar
• Psarra AM, Sekeris CE. Glucocorticoids induce mitochondrial gene transcription in HepG2 cells: role of the mitochondrial glucocorticoid receptor. Biochim Biophys Acta. 2011;1813:1814–1821.
   PubMed Web of Science ®Google Scholar
• Du J, Wang Y, Hunter R, et al. Dynamic regulation of mitochondrial function by glucocorticoids. Proc Natl Acad Sci USA. 2009;106:3543–3548.
   PubMed Web of Science ®Google Scholar
• Zhong DT, Shi CM, Chen Q, et al. Etoposide, vincristine, doxorubicin and dexamethasone (EVAD) combination chemotherapy as second-line treatment for advanced AIDS-related Kaposi’s sarcoma. J Cancer Res Clin Oncol. 2012;138:425–430.
   PubMed Web of Science ®Google Scholar
• Jing D, Bhadri VA, Beck D, et al. Opposing regulation of BIM and BCL2 controls glucocorticoid-induced apoptosis of pediatric acute lymphoblastic leukemia cells. Blood. 2015;125:273–283.
   PubMed Web of Science ®Google Scholar
• Huang Y, Zhou J, Huang Y, et al. SARI, a novel target gene of glucocorticoid receptor, plays an important role in dexamethasone-mediated killing of B lymphoma cells. Cancer Lett. 2016;373:57–66.
   PubMed Web of Science ®Google Scholar
• Ploner C, Schmidt S, Presul E, et al. Glucocorticoid-induced apoptosis and glucocorticoid resistance in acute lymphoblastic leukemia. J Steroid Biochem Mol Biol. 2005;93:153–160.
   PubMed Web of Science ®Google Scholar
• Lambrou GI, Vlahopoulos S, Papathanasiou C, et al. Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: relation to early gene expression. Leuk Res. 2009;33:1684–1695.
   PubMed Web of Science ®Google Scholar
• Herold MJ, McPherson KG, Reichardt HM. Glucocorticoids in T cell apoptosis and function. Cell Mol Life Sci. 2006;63:60–72.
   PubMed Web of Science ®Google Scholar
• Frankfurt O, Rosen ST. Mechanisms of glucocorticoid-induced apoptosis in hematologic malignancies: updates. Curr Opin Oncol. 2004;16:553–563.
   PubMed Web of Science ®Google Scholar
• Kfir-Erenfeld S, Yefenof E. Non-genomic events determining the sensitivity of hemopoietic malignancies to glucocorticoid-induced apoptosis. Cancer Immunol Immunother. 2014;63:37–43.
   PubMed Web of Science ®Google Scholar
• Conzen SD. Recent advances in understanding glucocorticoid receptor function in cancer. Clin Adv Hematol Oncol. 2017;15:338–340.
   PubMed Web of Science ®Google Scholar
• Volden PA, Conzen SD. The influence of glucocorticoid signaling on tumor progression. Brain Behav Immun. 2013;30(Suppl):S26–S31.
   PubMed Web of Science ®Google Scholar
• Sherlock P, Hartmann WH. Adrenal steroids and the pattern of metastases of breast cancer. JAMA. 1962;181:313–317.
   PubMed Web of Science ®Google Scholar
• Iversen HG, Hjort GH. The influence of corticoid steroids on the frequency of spleen metastases in patients with breast cancer. Acta Pathol Microbiol Scand. 1958;44:205–212.
   PubMedGoogle Scholar
• Wang H, Li M, Rinehart JJ, et al. Pretreatment with dexamethasone increases antitumor activity of carboplatin and gemcitabine in mice bearing human cancer xenografts: in vivo activity, pharmacokinetics, and clinical implications for cancer chemotherapy. Clin Cancer Res. 2004;10:1633–1644.
   PubMed Web of Science ®Google Scholar
• Wang H, Wang Y, Rayburn ER, et al. Dexamethasone as a chemosensitizer for breast cancer chemotherapy: potentiation of the antitumor activity of adriamycin, modulation of cytokine expression, and pharmacokinetics. Int J Oncol. 2007;30:947–953.
   PubMed Web of Science ®Google Scholar
• Reichardt HM, Kaestner KH, Tuckermann J, et al. DNA binding of the glucocorticoid receptor is not essential for survival. Cell. 1998;93:531–541.
   PubMed Web of Science ®Google Scholar
• Schacke H, Docke WD, Asadullah K. Mechanisms involved in the side effects of glucocorticoids. Pharmacol Ther. 2002;96:23–43.
   PubMed Web of Science ®Google Scholar
• Ayroldi E, Macchiarulo A, Riccardi C. Targeting glucocorticoid side effects: selective glucocorticoid receptor modulator or glucocorticoid-induced leucine zipper? A perspective. Faseb J. 2014;28:5055–5070.
   PubMed Web of Science ®Google Scholar
• Walker BR, Andrew R. Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease. Ann N Y Acad Sci. 2006;1083:165–184.
   PubMed Web of Science ®Google Scholar
• Kroon J, Koorneef LL, van den Heuvel JK, et al. Selective glucocorticoid receptor antagonist CORT125281 activates brown adipose tissue and alters lipid Distribution in male mice. Endocrinology. 2018;159:535–546.
   PubMed Web of Science ®Google Scholar
• Meyer M, Gonzalez Deniselle MC, Hunt H, et al. The selective glucocorticoid receptor modulator CORT108297 restores faulty hippocampal parameters in Wobbler and corticosterone-treated mice. J Steroid Biochem Mol Biol. 2014;143:40–48.
   PubMed Web of Science ®Google Scholar
• Zalachoras I, Houtman R, Atucha E, et al. Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator. Proc Natl Acad Sci USA. 2013;110:7910–7915.
   PubMed Web of Science ®Google Scholar
• van den Heuvel JK, Boon MR, van Hengel I, et al. Identification of a selective glucocorticoid receptor modulator that prevents both diet-induced obesity and inflammation. Br J Pharmacol. 2016;173:1793–1804.
   PubMed Web of Science ®Google Scholar
• Pineau F, Canet G, Desrumaux C, et al. New selective glucocorticoid receptor modulators reverse amyloid-beta peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109–122.
   PubMed Web of Science ®Google Scholar
• Vendruscolo LF, Estey D, Goodell V, et al. Glucocorticoid receptor antagonism decreases alcohol seeking in alcohol-dependent individuals. J Clin Invest. 2015;125:3193–3197.
   PubMed Web of Science ®Google Scholar
• Puhr M, Hoefer J, Eigentler A, et al. The glucocorticoid receptor is a key player for prostate cancer cell survival and a target for improved antiandrogen therapy. Clin Cancer Res. 2018;24:927–938.
   PubMed Web of Science ®Google Scholar
• Hunt H, inventor; Corcept Therapeutics, Inc., assignee. Glucocorticoid receptor modulators to treat cervical cancer. Patent WO 2018/183947 A1. 2018 Oct 4.
   Google Scholar
• Clark R, Ray N, Blaney N, et al., inventor; Corcept Therapeutics, Inc., assignee. Fused Ring Azadecalin Glucocorticoid Receptor Modulators. Patent US 2007/0281928 A1. 2007 Dec 6.
   Google Scholar
• Hunt H, Walters I, Ray N, inventor; Corcept Therapeutics, Inc., assignee. Heteroaryl-Ketone Fused Azadecalin Glucocorticoid Receptor Modulators. Patent US 2014/0038926 A1. 2014 Feb 6.
   Google Scholar
• Scott I, Tian W, Mains J, et al., inventor; Corcept Therapeutics, Inc., assignee. Octahydro fused azadecalin glucocorticoid receptor modulators. Patent US 2015/0148341 A1. 2015 May 28.
   Google Scholar
• Stites D, Abba I. Basic and clinical pharmacology. Norwalk (Conn): Appleton & Lange; 1991.
   Google Scholar
• Maggio ET. Enzyme immunoassay. Boca Raton (US): CRC Press; 2017.
   Google Scholar
• Tijssen P. Practice and theory of enzyme immunoassays. 1st ed. Laboratory techniques in biochemistry and molecular biology. Vol. 15. Amsterdam (NL): Elsevier Science; 1985.
   Google Scholar
• Choi SJ, Heiman AS, Lee HJ. Enzyme induction and receptor-binding affinity of steroidal 20-carboxamides in rat hepatoma tissue culture cells. Steroids. 1992;57:313–318.
   PubMed Web of Science ®Google Scholar
• Alexandrova M, Farkas P. Stress-induced changes of glucocorticoid receptor in rat liver. J Steroid Biochem Mol Biol. 1992;42:493–498.
   PubMed Web of Science ®Google Scholar
• Jones TR, Bell PA. Glucocorticoid-receptor interactions. Discrimination between glucocorticoid agonists and antagonists by means of receptor-binding kinetics. Biochem J. 1982;204:721–729.
   PubMed Web of Science ®Google Scholar
• Dausse JP, Duval D, Meyer P, et al. The relationship between glucocorticoid structure and effects upon thymocytes. Mol Pharmacol. 1977;13:948–955.
   PubMed Web of Science ®Google Scholar
• Teutsch JG, Costerousse G, Philbert D, et al., inventor; Population Council, Inc., assignee. Novel steroids. Patent US 1983/4386085 A. 1983 May 31.
   Google Scholar
• Bocquel MT, Ji J, Ylikomi T, et al. Type II antagonists impair the DNA binding of steroid hormone receptors without affecting dimerization. J Steroid Biochem Mol Biol. 1993;45:205–215.
   PubMed Web of Science ®Google Scholar
• Van Raemdonck GA, Tjalma WA, Coen EP, et al. Identification of protein biomarkers for cervical cancer using human cervicovaginal fluid. PLoS One. 2014;9:e106488.
   PubMed Web of Science ®Google Scholar
• Kang H, Lee HY, Lee KS, et al. Imaging-based tumor treatment response evaluation: review of conventional, new, and emerging concepts. Korean J Radiol. 2012;13:371–390.
   PubMed Web of Science ®Google Scholar
• Eisenhauer EA, Therasse P, Bogaerts J, et al. New response evaluation criteria in solid tumours: revised RECIST guideline (version 1.1). Eur J Cancer. 2009;45:228–247.
   PubMed Web of Science ®Google Scholar
• Hunt H, Block T, inventor; Corcept Therapeutics, Inc., assignee. Glucocorticoid receptor modulators to treat pancreatic cancer. Patent WO 2018/049255 A1. 2018 Mar 15.
   Google Scholar
• Hunt H, inventor; Corcept Therapeutics, Inc., assignee. The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors. Patent WO 2017/151613. 2017 Sept 8.
   Google Scholar
• Moraitis A, inventor; Corcept Therapeutics, Inc., assignee. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators. Patent WO 2018/236749. 2018 Dec 27.
   Google Scholar
• Toren A, Reichardt JK, Andalibi A, et al. Novel age-dependent targets in vestibular schwannomas. Hum Genomics. 2014;8:10.
   PubMed Web of Science ®Google Scholar
• Moraitis A, inventor; Corcept Therapeutics, Inc., assignee. Use of glucocorticoid receptor modulators in the treatment of catecholamine-secreting tumors. Patent WO 2018/165460. 2018 Sept 13.
   Google Scholar
• Grouzmann E, Tschopp O, Triponez F, et al. Catecholamine metabolism in paraganglioma and pheochromocytoma: similar tumors in different sites? PLoS One. 2015;10:e0125426.
   PubMed Web of Science ®Google Scholar
• Goodman R, Edgar D, Thoenen H, et al. Glucocorticoid induction of tyrosine hydroxylase in a continuous cell line of rat pheochromocytoma. J Cell Biol. 1978;78:R1–R7.
   PubMed Web of Science ®Google Scholar
• Solomon MB, Wulsin AC, Rice T, et al. The selective glucocorticoid receptor antagonist CORT 108297 decreases neuroendocrine stress responses and immobility in the forced swim test. Horm Behav. 2014;65:363–371.
   PubMed Web of Science ®Google Scholar
• K urzG, Camacho Gómez J, et al., inventor; Oncostellae, S.L., assignee. New analogs as androgen receptor and glucocorticoid receptor modulators. Patent WO 2019/086720 A1. 2019 May 9.
   Google Scholar
• Watson PA, Arora VK, Sawyers CL. Emerging mechanisms of resistance to androgen receptor inhibitors in prostate cancer. Nat Rev Cancer. 2015;15:701–711.
   PubMed Web of Science ®Google Scholar
• Du X, Eksterowicz J, Fantin V, et al., inventor; Oric Pharmaceuticals, Inc., assignee. Glucocorticoid receptor modulators. Patent WO 2018/191283 A1. 2018 Oct 18.
   Google Scholar
• Pirmohamed M, James S, Meakin S, et al. Adverse drug reactions as cause of admission to hospital: prospective analysis of 18 820 patients. BMJ. 2004;329:15–19.
   PubMed Web of Science ®Google Scholar
• Hunt HJ, Belanoff JK, Walters I, et al. Identification of the clinical candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexah ydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methano ne (CORT125134): a selective Glucocorticoid Receptor (GR) antagonist. J Med Chem. 2017;60:3405–3421.
   PubMed Web of Science ®Google Scholar
• Hunt HJ, Belanoff JK, Golding E, et al. 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. Bioorg Med Chem Lett. 2015;25:5720–5725.
   PubMed Web of Science ®Google Scholar
• Clark RD, Ray NC, Williams K, et al. 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. Bioorg Med Chem Lett. 2008;18:1312–1317.
   PubMed Web of Science ®Google Scholar
• Christodoulou MS, Dapiaggi F, Ghiringhelli F, et al. Imidazo[2,1-b]benzothiazol derivatives as potential allosteric inhibitors of the glucocorticoid receptor. ACS Med Chem Lett. 2018;9:339–344.
   PubMed Web of Science ®Google Scholar
• Rew Y, Du X, Eksterowicz J, et al. Discovery of a potent and selective steroidal glucocorticoid receptor antagonist (ORIC-101). J Med Chem. 2018;61:7767–7784.
   PubMedGoogle Scholar
• Sun D, McGee L, Du X, et al. inventor; Oric Pharmaceuticals, Inc., assignee. Inhibitors of glucocorticoid receptor. Patent WO 2017/112902. 2017 Jun 29.
   Google Scholar
• Kondo J, Inoue M. Application of Cancer Organoid Model for Drug Screening and Personalized Therapy. Cells. 2019;8:470.
   PubMed Web of Science ®Google Scholar
• Genova E, Cavion F, Lucafò M, et al. Induced pluripotent stem cells for therapy personalization in pediatric patients: Focus on drug-induced adverse events. World J Stem Cells. 2019;11:1020–1044.
   PubMed Web of Science ®Google Scholar