Tìm theo
Dasatinib
Các tên gọi khác (8 ) :
  • Anh. dasatinib
  • Anhydrous dasatinib
  • BMS dasatinib
  • BMS-354825
  • Dasatinib
  • Dasatinib (anh.)
  • Dasatinibum
  • N-(2-CHLORO-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
Thuốc Gốc
Small Molecule
CAS: 302962-49-8
ATC: L01XE06
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C22H26ClN7O2S
PTK: 488.006
Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H26ClN7O2S
Phân tử khối
488.006
Monoisotopic mass
487.155721508
InChI
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
InChI Key
InChIKey=ZBNZXTGUTAYRHI-UHFFFAOYSA-N
IUPAC Name
N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
Traditional IUPAC Name
dasatinib
SMILES
CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1
Độ tan chảy
280-286 °C
Độ hòa tan
1.28e-02 g/l
logP
1.8
logS
-4.6
pKa (strongest acidic)
8.49
pKa (Strongest Basic)
7.22
PSA
106.51 Å2
Refractivity
133.08 m3·mol-1
Polarizability
51.58 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
8
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor
Cơ Chế Tác Dụng : Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
Dược Động Học :

▧ Volume of Distribution :
* 2505 L
▧ Protein binding :
96%
▧ Metabolism :
Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4
▧ Route of Elimination :
Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces.
▧ Half Life :
The overall mean terminal half-life of dasatinib is 3-5 hours.
Độc Tính : Acute overdose in animals was associated with cardiotoxicity.
Chỉ Định : For the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Eptifibatide Monitor therapy due to enhanced anticoagulant effect.
  • Etravirine Dasatinib, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid this combination if possible. If concurrent therapy cannot be avoided it is recommended to increase the dose of dasitinib and monitor for efficacy and toxicity.
  • Omeprazole Omeprazole may decrease the serum level of dasatinib.
  • Pantoprazole Pantoprazole may decrease the serum level of dasatinib.
  • Phenobarbital Phenobarbital may decrease the serum level and efficacy of dasatinib.
  • Phenytoin Phenytoin may decrease the serum level and efficacy of dasatinib.
  • Rabeprazole Rabeprazole may decrease the serum level of dasatinib.
  • Ranitidine Ranitidine may decrease the serum level of dasatinib.
  • Rifampicin Rifampin may decrease the serum level and efficacy of dasatinib.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telithromycin Telithromycin may reduce clearance of Dasatinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dasatinib if Telithromycin is initiated, discontinued or dose changed.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Voriconazole Additive QTc prolongation may occur. Voriconazole, a strong CYP3A4 inhibitor, may also increase the serum concentration of dasatinib by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of dasatinib if voriconazole is initiated, discontinued or dose changed.
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Sprycel 20 mg tablet
    Giá bán buôn : USD >69.56
    Đơn vị tính : tablet
  • Biệt dược thương mại : Sprycel 50 mg tablet
    Giá bán buôn : USD >139.12
    Đơn vị tính : tablet
  • Biệt dược thương mại : Sprycel 70 mg tablet
    Giá bán buôn : USD >139.12
    Đơn vị tính : tablet
  • Biệt dược thương mại : Sprycel 100 mg tablet
    Giá bán buôn : USD >278.24
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Sprycel
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01254
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3062316
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505143
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03658
ChemSpider
http://www.chemspider.com/Chemical-Structure.2323020.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=13216
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0003-0527-11
PharmGKB
http://www.pharmgkb.org/drug/PA162372878
Wikipedia
http://en.wikipedia.org/wiki/Dasatinib
RxList
http://www.rxlist.com/cgi/generic/sprycel.htm
Drugs.com
http://www.drugs.com/cdi/dasatinib.html
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