References
- BRANDSTETTER, H., KEHENE, A., BODE, W., HUBER,. R., VON DER SAAL, W., WIRTHENSOHN, K. and ENGH R. A., 1996, X-ray structure of active site-inhibited clotting factor Xa. Journal of Biological Chemistry, 271, 29988–29992.
- DAVIES, B. and MORRIS, T., 1993, Physiological parameters in laboratory animals and humans. Pharmaceutical Research, 10, 1093–1095.
- HARA, T., MORISHIMA, Y., IsmitAkA, H., MURAYAMA, N., TANAKA, S., SUDO, K. and KUNITADA, S., 1995a, Inhibition of thrombin generation effectively prevents thrombus formation without aggravation of bleeding. Thrombosis and Haemostasis, 73, 1308.
- HARA, T., YOKOYAMA, A., IsmitAkA, H., YOKOYAMA, Y., NAGAHARA, T. and IwAmoto, M., 1994, DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thrombosis and Haemostasis, 71, 314–319.
- HARA, T., YOKOYAMA, A., TANABE, K., IsmitAkA, H. and IwAmoto, M., 1995b, DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thrombosis and Haemostasis, 74,635–639.
- IKEDA, Y., FuttA, M., MURAYAMA, N., YAMADA, H., INouE, T., SASANO, H. and KUNITADA, S., 1998, Human pharmacokinetics, pharmacodynamics, and tolerability of activated factor Xa inhibitor DX-9065a. Circulation, 98(suppl.), 1454.
- LIN, Z. and JOHNSON, M. E., 1995, Proposed cation-ir mediated binding by factor Xa: a novel enzymatic mechanism for molecular recognition. FEBS Letters, 370, 1–5.
- MORISHIMA, Y., TANABE, K., TERADA, Y., HARA, T. and KUNITADA, S., 1997, Antithrombotic and hemorrhagic effects of DX-9065a, a direct and selective factor Xa inhibitor: comparison with a direct thrombin inhibitor and antithrombin III-dependent anticoagulants. Thrombosis and Haemostasis, 78, 1366–1371.
- MURAYAMA, N., TANAKA, S., KIKUCHI, T., NAKAOKA, M. and SUDO, K. 1996, Radioimmunoassay method for DX-9065a, an anticoagulant agent. Development, evaluation and application to human plasma. Journal of Pharmaceutical and Biomedical Analysis, 14, 1435–1445.
- MURAYAMA, N., TANAKA, M., KUNITADA, S., YAMADA, H., INouE, T., TERADA, Y., FUJTTA, M. and IKEDA, Y., 1999, Tolerability, pharmacokinetics and pharmacodynamics of DX-9065a, a new synthetic, potent and specific factor Xa inhibitor, in healthy male volunteers. Clinical Pharmacology and Therapeutics, 66, 258–264.
- STUBBS, M. T., HUBER, R. and BODE, W., 1995, Crystal structures of factor Xa specific inhibitors in complex with trypsin: structural grounds for inhibition of factor Xa and selectivity against thrombin. FEBS Letters, 375, 103–107.