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Publications

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  1. Roche M, Kyriakou H, Seiden M: Drug evaluation: tesetaxel − an oral semisynthetic taxane derivative. Curr Opin Investig Drugs 7:1092-9, 2006.

  2. Ono C, Takao A, Atsumi R: Absorption, distribution, and excretion of DJ-927, a novel orally effective taxane, in mice, dogs, and monkeys. Biol Pharm Bull 27:345-51, 2004.

  3. Shionoya M, et al.: DJ-927, a novel oral taxane, overcomes P-glycoprotein-mediated multidrug resistance in vitro and in vivo. Cancer Sci 94:459-66, 2003.

  4.  Beeram M, et al.: A Phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of the combination of an oral antimicrotubular agent, DJ-927 (D), and capecitabine (C) in patients (pts) with advanced cancers. Proc Am Soc Clin Oncol 24:83s, 2006.

  5.  Syed SK, et al.: Phase I and pharmacokinetics (PK) of DJ-927, an oral taxane, in patients (pts) with advanced cancers. Proc Am Soc Clin Oncol 22:134, 2004.

  6. Moore MR, et al.: Phase II trial of DJ-927, an oral tubulin depolymerization inhibitor, in the treatment of metastatic colorectal cancer. Proc Am Soc Clin Oncol 24:168s, 2006.

  7. Rhee JM, et al.: Phase II trial of DJ-927 as a second-line treatment for colorectal cancer demonstrates objective responses. Proc Am Soc Clin Oncol 23:284s, 2005.

  8. Szczesna A, et al.: A Phase II study of DJ-927 administered orally once every three weeks as a second line therapy to subjects with locally advanced or metastatic non small cell lung cancer after failure of platinum-based non-taxane regimen. Proc Am Soc Clin Oncol 24:667s, 2006.

  9. Evans T, et al.: A Phase II study of DJ-927 as second-line therapy in patients (pts) with advanced gastric cancer (GC) who have failed a 5-FU non taxane based regimen. Proc Am Soc Clin Oncol 24:18s, 2006.
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Mechanism of Action

Tesetaxel stabilizes cytoskeletal structures known as microtubules. This mechanism is common to all taxanes, and it induces potent cytotoxic effects in a wide range of tumor cell types.

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Clinical Development

To date, oral tesetaxel has been studied in Phase 1 and Phase 2 studies involving more than 280 patients.

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