11)
社内資料：イマチニブ抵抗性の慢性期又は移行期CML患者に対する外国第II相試験　〔TASU00022〕

12)
社内資料：細胞株を用いた測定系による選択的阻害作用　〔TASU00011〕

13)
社内資料：Bcr-Abl変異体に対する自己リン酸化阻害、細胞増殖阻害　〔TASU00012〕

14)
社内資料：BCR-ABL遺伝子導入細胞を静脈内移植したマウスに対する抗腫瘍効果　〔TASU00013〕

15)
社内資料：Ablキナーゼに対する阻害様式　〔TASU00014〕

16)
Fiskus,W.et al.：Blood 108（2）,645,2006　〔TASM00057〕

17)
Manley,P.W.et al.：Biochim.Biophys.Acta 1754（1-2）,3,2005　〔TASS00001〕

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ノバルティスファーマ株式会社　ノバルティスダイレクト

〒105-6333 東京都港区虎ノ門1-23-1

製造販売業者等の氏名又は名称及び住所

製造販売
ノバルティス ファーマ株式会社

東京都港区虎ノ門1-23-1
Tasigna(nilotinib Capsules)
WARNING
QT PROLONGATION AND SUDDEN DEATHS
•Tasigna prolongs the QT interval. Prior to Tasigna administration and periodically, monitor for hypokalemia or hypomagnesemia and correct deficiencies (see WARNINGS AND PRECAUTIONS). Obtain ECGs to monitor the QTc at baseline, seven days after initiation, and periodically thereafter, and follow any dose adjustments.
•Sudden deaths have been reported in patients receiving nilotinib (see WARNINGS AND PRECAUTIONS). Do not administer Tasigna to patients with hypokalemia, hypomagnesemia, or long QT syndrome (see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS).
•Avoid use of concomitant drugs known to prolong the QT interval and strong CYP3A4 inhibitors.
•Patients should avoid food 2 hours before and 1 hour after taking dose (see WARNINGS AND PRECAUTIONS).
DRUG DESCRIPTION
Tasigna (nilotinib) belongs to a pharmacologic class of drugs known as kinase inhibitors.
Nilotinib drug substance, a monohydrate monohydrochloride, is a white to slightly yellowish to slightly greenish yellow powder with the anhydrous molecular formula and weight, respectively, of C28H22F3N7O•HCl• H2O and 584. The solubility of nilotinib in aqueous solutions decreases with increasing pH. Nilotinib is notoptically active. The pKa1 was determined to be 2.1; pKa2 was estimated to be 5.4.
The chemical name of nilotinib is 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide, monohydrochloride, monohydrate. Its structure is shown below:
Tasigna (nilotinib) Capsules, For Oral Use, contain 150 mg or 200 mg nilotinib base, anhydrous (as hydrochloride, monohydrate) with the following inactive ingredients: colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate and polyoxamer 188. The capsules contain gelatin, iron oxide (red), iron oxide (yellow), iron oxide (black) and titanium dioxide.
What are the possible side effects of nilotinib (Tasigna)?
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Stop using nilotinib and call your doctor at once if you have a serious side effect such as:
•feeling like you might pass out, fast or pounding heartbeat, seizure (convulsions);
•pale skin, weakness, feeling light-headed, rapid heart rate, trouble concentrating;
•easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin;
•fever, chills, body.
Read All Potential Side Effects and See Pictures of Tasigna Capsules »