ニロチニブ

nilotinib
タシグナ
開発名
AMN107
mab達


  • チロシンキナーゼ阻害薬

効能又は効果

  • イマチニブ抵抗性の慢性期又は移行期の慢性骨髄性白血病(タシグナカプセル200mg)

添付文書

  • タシグナカプセル200mg
<click2in>http://www.info.pmda.go.jp/go/pack/4291021M1020_1_04/4291021M1020_1_04?view=body</click2in>

文献

  • E. Weisberg, P.W. Manley and W. Breitenstein et al., Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl, Cancer Cell 7 (2005), pp. 129-141, PMID 19467857
nilotinib (formerly AMN107), a second-generation oral TKI, engineered to specifically inhibit KIT, PDGFRa and BCR-ABL.
Smaller phase I/II trials or retrospective series have suggested efficacy of nilotinib(22),

sorafenib(33,34) and IPI-504(35) after imatinib and/or sunitinib failure.

nilotinib 22,
22. Blay JY, Casali PG, Reichardt P, et al. A phase I study of

nilotinib alone and in combination with imatinib in patients with imatinib-resistant gastrointestinal stromal tumors (GIST): study update. J Clin Oncol 2008:26. Abstract 10553.

sorafenib 33,34
33. Gelderblom H, Montemurro M, Schu¨ tte J, et al. Sorafenib

fourth-line treatment in imatinib, sunitinib, and nilotinib resistant metastatic GIST: a retrospective analysis. ASCO Gastrointestinal Cancers Symposium 2009; [Abstract 51].

抄録が存在しない
34. Wiebe L, Kasza KE, Maki RG, et al. Activity of sorafenib (SOR)

in patients (pts) with imatinib (IM) and sunitinib (SU)- resistant (RES) gastrointestinal stromal tumors (GIST): a phase II trial of the University of Chicago Phase II Consortium. J Clin Oncol 2008:26. Abstract 10502.

抄録が存在しない
IPI-504 35
35. Wagner AJ, Morgan JA, Chugh R, et al. Inhibition of heat shock

protein 90 (Hsp90) with the novel agent IPI-504 in metastatic GIST following failure of tyrosine kinase inhibitors (TKIs) or other sarcomas: clinical results from phase I trial. ASCO Meeting Abstracts 2008;26 [Abstract 10503].

  • Schlemmer M, Schinwald N, Bruns C, Berger F, Reichardt P., Response to Nilotinib as a First-Line Treatment for Metastatic Gastrointestinal Stromal Tumors., J Gastrointest Cancer. 2010 Oct 5. [Epub ahead of print]; PMID 20922581
ONCLUSION: This is the first report demonstrating the feasibility of nilotinib (400 mg bid) for the first-line treatment of metastatic GIST. Furthermore, these results underscore that responses to TKIs may be underestimated by Response Evaluation Criteria in Solid Tumors.