Metabolic disposition of AZD8931, an oral equipotent inhibitor of EGFR, HER2 and HER3 signalling, in rat, dog and man

References

• Alvarez JV, Greulich H, Sellers WR, et al. (2006). Signal transducer and activator of transcription 3 is required for the oncogenic effects of non-small-cell lung cancer-associated mutations of the epidermal growth factor receptor. Cancer Res 66:3162–8
   PubMed Web of Science ®Google Scholar
• AstraZeneca. Global Policy: Bioethics. 2011. Available at: http://www.astrazeneca.com/Responsibility/Code-policies-standards/Our-global-policies [last accessed Jul 2013].
   Google Scholar
• Atrakchi AH. (2009). Interpretation and considerations on the safety evaluation of human drug metabolites. Chem Res Toxicol 22:1217–20
   PubMed Web of Science ®Google Scholar
• Baillie TA, Cayen MN, Fouda H, et al. (2002). Drug metabolites in safety testing. Toxicol Appl Pharmacol 182:188–96
   PubMed Web of Science ®Google Scholar
• Baselga J, Hegg R, Losada MV, et al. (2013). A Phase II randomized placebo-controlled study of AZD8931, an inhibitor of EGFR, HER2 and HER3 signaling, plus paclitaxel (P) vs P alone in patients (pts) with low HER2-expressing advanced breast cancer (BC) (THYME). Proceedings of the American Association for Cancer Research Abstract LB-146, Washington Convention Center, Washington, DC
   Google Scholar
• Baselga J, Swain SM. (2009). Novel anticancer targets: revisiting ERBB2 and discovering ERBB3. Nat Rev Cancer 9:463–75
   PubMed Web of Science ®Google Scholar
• Ciardiello F, Tortora G. (2008). EGFR antagonists in cancer treatment. N Engl J Med 358:1160–74
   PubMed Web of Science ®Google Scholar
• Citri A, Yarden Y. (2006). EGF-ERBB signalling: towards the systems level. Nat Rev Mol Cell Biol 7:505–16
   PubMed Web of Science ®Google Scholar
• Cully M, You H, Levine AJ, Mak TW. (2006). Beyond PTEN mutations: the PI3K pathway as an integrator of multiple inputs during tumorigenesis. Nat Rev Cancer 6:184–92
   PubMed Web of Science ®Google Scholar
• DiGiovanna MP, Stern DF, Edgerton SM, et al. (2005). Relationship of epidermal growth factor receptor expression to ErbB-2 signaling activity and prognosis in breast cancer patients. J Clin Oncol 23:1152–60
   PubMed Web of Science ®Google Scholar
• Engelman JA, Cantley LC. (2006). The role of the ErbB family members in non-small cell lung cancers sensitive to epidermal growth factor receptor kinase inhibitors. Clin Cancer Res 12:4372s–6s
   Google Scholar
• Engelman JA, Zejnullahu K, Mitsudomi T, et al. (2007). MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316:1039–43
   PubMed Web of Science ®Google Scholar
• European Medicines Agency (EMA). (2002). ICH topic E6(R1): Guideline for good clinical practice. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use. July. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002874.pdf [last accessed Jul 2014]
   Google Scholar
• FDA Guideline for Industry. (2005). Pharmacokinetics: guidance for repeated dose tissue distribution studies. Available at: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm074938.pdf [last accessed Jul 2013]
   Google Scholar
• Fukuoka M, Yano S, Giaccone G, et al. (2003). Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer. J Clin Oncol 21:2237–46
   PubMed Web of Science ®Google Scholar
• Hamilton RA, Garnett WR, Kline BJ. (1981). Determination of mean valproic acid serum level by assay of a single pooled sample. Clin Pharmacol Ther 29:408–13
   PubMed Web of Science ®Google Scholar
• Hickinson DM, Klinowska T, Speake G, et al. (2010). AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res 16:1159–69
   PubMed Web of Science ®Google Scholar
• Hubbard SR. (2009). The juxtamembrane region of EGFR takes center stage. Cell 137:1181–3
   PubMed Web of Science ®Google Scholar
• Hynes NE, Horsch K, Olayioye MA, Badache A. (2001). The ErbB receptor tyrosine family as signal integrators. Endocr Relat Cancer 8:151–9
   PubMed Web of Science ®Google Scholar
• Hynes NE, Lane HA. (2005). ERBB receptors and cancer: the complexity of targeted inhibitors. Nat Rev Cancer 5:341–54
   PubMed Web of Science ®Google Scholar
• Johnston SRD, Basik M, Hegg R, et al. (2013). Phase II randomized study of the EGFR, HER2, HER3 signaling inhibitor AZD8931 in combination with anastrozole (A) in women with endocrine therapy (ET) naive advanced breast cancer (MINT). J Clin Oncol (Meeting Abstracts) 31(15 Suppl):531
   Web of Science ®Google Scholar
• Jorissen RN, Walker F, Pouliot N, et al. (2003). Epidermal growth factor receptor: mechanisms of activation and signalling. Exp Cell Res 284:31–53
   PubMed Web of Science ®Google Scholar
• Kapitanovic S, Radosevic S, Slade N, et al. (2000). Expression of erbB-3 protein in colorectal adenocarcinoma: correlation with poor survival. J Cancer Res Clin Oncol 126:205–11
   PubMed Web of Science ®Google Scholar
• Kosaka T, Yamaki E, Mogi A, Kuwano H. (2011). Mechanisms of resistance to EGFR TKIs and development of a new generation of drugs in non-small-cell lung cancer. J Biomed Biotechnol 2011:165214 . doi: 10.1155/2011/165214
   PubMed Web of Science ®Google Scholar
• Kris MG, Natale RB, Herbst RS, et al. (2003). Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. JAMA 290:2149–58
   PubMed Web of Science ®Google Scholar
• Leblanc B, Jezequel S, Davies T, et al. (1998). Binding of drugs to eye melanin is not predictive of ocular toxicity. Regul Toxicol Pharmacol 28:124–32
   PubMed Web of Science ®Google Scholar
• Lee-Hoeflich ST, Crocker L, Yao E, et al. (2008). A central role for HER3 in HER2-amplified breast cancer: implications for targeted therapy. Cancer Res 68:5878–87
   PubMed Web of Science ®Google Scholar
• Legraverend C, Mode A, Westin S, et al. (1992). Transcriptional regulation of rat P-450 2C gene subfamily members by the sexually dimorphic pattern of growth hormone secretion. Mol Endocrinol 6:259–66
   PubMed Web of Science ®Google Scholar
• Lin JH, Chiba M, Chen IW, et al. (1996). Sex-dependent pharmacokinetics of indinavir: in vivo and in vitro evidence. Drug Metab Dispos 24:1298–306
   PubMed Web of Science ®Google Scholar
• Liu Z, Carvajal M, Carraway CA, et al. (2001). Expression of the receptor tyrosine kinases, epidermal growth factor receptor, ErbB2, and ErbB3, in human ocular surface epithelia. Cornea 20:81–5
   PubMed Web of Science ®Google Scholar
• Lopez-Martin JA, Vidal Losada M, Cortes J, et al. (2011). Phase I, dose-finding study of AZD8931, an inhibitor of ErbB1, 2 and 3 receptor signaling, in combination with paclitaxel (P). J Clin Oncol 29(15 Suppl): 3105
   PubMed Web of Science ®Google Scholar
• Medina PJ, Goodin S. (2008). Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther 30:1426–47
   PubMed Web of Science ®Google Scholar
• Nicholson RI, Gee JM, Harper ME. (2001). EGFR and cancer prognosis. Eur J Cancer 37:S9–15
   PubMed Web of Science ®Google Scholar
• Perez-Soler R. (2003). Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome? Oncology (Huntington) 17:23–8
   PubMedGoogle Scholar
• Renouf DJ, Velazquez-Martin JP, Simpson R, et al. (2012). Occular toxicity of targeted therapies. J Clin Oncol 30:3277–86
   Google Scholar
• Salomon D, Gullick W. (2001). The erbB family of receptors and their ligands: multiple targets for therapy. Signal 2:4–11
   Google Scholar
• Sjogren S, Inganas M, Lindgren A, et al. (1998). Prognostic and predictive value of c-erbB-2 overexpression in primary breast cancer, alone and in combination with other prognostic markers. J Clin Oncol 16:462–9
   PubMed Web of Science ®Google Scholar
• Smith DA, Obach RS. (2006). Metabolites and safety: What are the concerns, and how should we address them? Chem Res Toxicol 19:1570–9
   PubMed Web of Science ®Google Scholar
• Smith DA, Obach RS. (2009). Metabolites in safety testing (MIST): considerations of mechanisms of toxicity with dose, abundance, and duration of treatment. Chem Res Toxicol 22:267–79
   PubMed Web of Science ®Google Scholar
• Tanner B, Hasenclever D, Stern K, et al. (2006). ErbB-3 predicts survival in ovarian cancer. J Clin Oncol 24:4317–23
   PubMed Web of Science ®Google Scholar
• Thompson KL, Vincent SH, Miller RR, et al. (1997). Pharmacokinetics and disposition of the oxytocin receptor antagonist L-368,899 in rats and dogs. Drug Metab Dispos 25:1113–18
   PubMed Web of Science ®Google Scholar
• Tjulandin S, Moiseyenko V, Semiglazov V, et al. (2014). Phase I, dose-finding study of AZD8931, an inhibitor of EGFR (erbB1), HER2 (erbB2) and HER3 (erbB3) signaling, in patients with advanced solid tumors. Invest New Drugs 32:145–53
   PubMed Web of Science ®Google Scholar
• Ullberg S, Larsson B. (1981). Whole body autoradiography. In: Bridges JW, Chasseaud LF, eds. Progress in drug metabolism, Vol. 6, Chapter 5. Chichester: John Wiley and Sons Ltd., 249–89
   Google Scholar
• vis-Bruno KL, Atrakchi A. (2006). A regulatory perspective on issues and approaches in characterizing human metabolites. Chem Res Toxicol 19:1561–3
   PubMed Web of Science ®Google Scholar
• Vokes EE, Chu E. (2006). Anti-EGFR therapies: clinical experience in colorectal, lung, and head and neck cancers. Oncology (Williston Park) 20:15–25
   PubMedGoogle Scholar
• Waxman DJ, Ram PA, Notani G, et al. (1990). Pituitary regulation of the male-specific steroid 6 beta-hydroxylase P-450 2a (gene product IIIA2) in adult rat liver. Suppressive influence of growth hormone and thyroxine acting at a pretranslational leve. Mol Endocrinol 4:447–54
   PubMed Web of Science ®Google Scholar
• World Medical Association (WMA). (1964). Declaration of Helsinki. Ethical principles for medical research involving human subjects. Adopted by the 18th WMA General Assembly, Helsinki, Finland, June. Available at: http://www.wma.net/en/30publications/10policies/b3/index.html [last accessed Jul 2013]
   Google Scholar
• Yi ES, Harclerode D, Gondo M, et al. (1997). High c-erbB-3 protein expression is associated with shorter survival in advanced non-small cell lung carcinomas. Mod Pathol 10:142–8
   PubMed Web of Science ®Google Scholar
• Zhang XL, Yang YS, Xu DP, et al. (2009). Comparative study on overexpression of HER2/neu and HER3 in gastric cancer. World J Surg 33:2112–18
   PubMed Web of Science ®Google Scholar