Preclinical pharmacokinetic, toxicological and biomarker evaluation of SR16157, a novel dual-acting steroid sulfatase inhibitor and selective estrogen receptor modulator

Cancer Chemotherapy and Pharmacology

Volumn 67, Issue 6, 2011, Pages 1341-1352

  Rausch, Linda ^a   Green, Carol ^a   Steinmetz, Karen ^a   LeValley, Sue ^a   Catz, Paul ^a   Zaveri, Nurulain ^a   Schweikart, Karen ^b   Tomaszewski, Joseph ^b   Mirsalis, Jon ^a  

^a SRI INTERNATIONAL   (United States)

^b NATIONAL CANCER INSTITUTE   (United States)

Author keywords

Biomarker; Breast cancer; Estrone sulfatase; SERM; Steroid sulfatase

Indexed keywords

BIOLOGICAL MARKER; NSC 732011; SELECTIVE ESTROGEN RECEPTOR MODULATOR; SR 16157; STERYL SULFATASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BIOAVAILABILITY; BLOOD CHEMISTRY; BODY WEIGHT; CONTROLLED STUDY; DOG; DOSE LIMITING TOXICITY; DRUG BIOAVAILABILITY; DRUG DOSE ESCALATION; DRUG HALF LIFE; DRUG RESPONSE; DRUG TOXICITY; ENZYME ACTIVITY; FEMALE; HEMATOLOGY; HISTOPATHOLOGY; IN VIVO STUDY; LIVER; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PRIORITY JOURNAL; SINGLE DRUG DOSE; TOXICOKINETICS;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS, HORMONAL; BIOLOGICAL AVAILABILITY; BIOLOGICAL MARKERS; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; LEUKOCYTES, MONONUCLEAR; MALE; NORPREGNATRIENES; RATS; RATS, INBRED F344; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SPECIES SPECIFICITY; STERYL-SULFATASE;

EID: 79959603986     PISSN: 03445704     EISSN: 14320843     Source Type: Journal    
DOI: 10.1007/s00280-010-1430-x     Document Type: Article

References (12)

1. Janicke F (2004) Are all aromatase inhibitors the same? A review of the current evidence. Breast 13:S10-S18
2. Santner SJ, Feil PD, Santen RJ (1984) In situ estrogen production via the estrone sulfatase pathway in breast tumors: relative importance versus the aromatase pathway. J Clin Endocrinol Metab 59:29-33
3. Adams J, Garcia M, Rochefort H (1981) Estrogenic effects of physiological concentrations of 5-androstene-3 beta, 17 beta-diol and its metabolism in MCF7 human breast cancer cells. Cancer Res 4(11 Pt):4720-4726 (Pubitemid 12201398)
4. Poulin R, Labrie F (1986) Stimulation of cell proliferation, estrogenic response by adrenal C19-delta 5-steroids in the ZR-73-1 human breast cancer cell line. Cancer Res 46(10):4933-4937 (Pubitemid 16008241)
5. Maggiolini M, Donze O, Jeannin E, Ando S, Picard D (1999) Adrenal androgens stimulate the proliferation of breast cancer cells as direct activators of estrogen receptor. Cancer Res 59:4864-4869 (Pubitemid 29472889)
6. Purohit A, Williams GJ, Howarth NM, Potter BV, Reed MJ (1995) Inactivation of steroid sulfatase by an active site-directed inhibitor, estrone-3-O-sulfamate. Biochemistry 34:11508-11514
7. Ciobanu LC, Boivin RP, Luu-The V, Poirier D (2001) Synthesis steroid sulphatase inhibitory activity of C19-and C21-steroidal derivatives bearing a benzyl-inhibiting group. Eur J Med Chem 36(7-8):659-671 (Pubitemid 32964736)
8. Stanway SJ, Purohit A, Woo LW, Sufi S, Vigushin D, Ward R, Wilson RH, Stanczyk FZ, Dobbs N, Kulinskaya E, Elliott M, Potter BV, Reed MJ, Coombes RC (2006) Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor. Clin Cancer Res 12(5):1585-1592
9. Zaveri N, Chao WR, Peters R, Tanabe M, Yamada Y, Toko T, Asao T, Eshima K (2003) A novel dual targeted approach for the endocrine therapy and prevention of breast cancer. SR16158, a novel steroid sulfatase inhibitor/tissue-selective antiestrogen SERM. Presented at American Association for Cancer Research Advances in Breast Cancer Symposium, Huntington Beach, CA
10. Rasmussen LM, Zaveri NT et al (2007) A novel dual-target steroid sulfatase inhibitor and antiestrogen: SR16157, a promising agent for the therapy of breast cancer. Breast Cancer Res Treat 106:191-203 (Pubitemid 350045017)
11. Doppalapudi RS, Riccio ES, Rausch LL et al (2007) Evaluation of chemopreventative agents for genotoxic activity. Mutat Res 629:148-160 (Pubitemid 46603083)
12. U.S. Federal Drug Administration (2003) FDA guidance for industry and reviewers estimating safe starting dose for therapeutics in adult healthy volunteers, FR vol 68, pp 2340-2341, 16 Jan 2003. Accessed 10 Oct 2009 from http://www.fda.gov/cber/gdlns/dose.htm