Tìm theo
Thiotepa
Các tên gọi khác (1) :
  • Thioplex
Thuốc Gốc
Small Molecule
CAS: 52-24-4
ATC: L01AC01
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C6H12N3PS
PTK: 189.218
N,N'N'-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. It is a stable derivative of N,N',N''- triethylenephosphoramide (TEPA). It is mostly used to treat breast cancer, ovarian cancer and bladder cancer. It is also used as conditioning for Bone marrow transplantation. Its main toxicity is myelosuppression.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H12N3PS
Phân tử khối
189.218
Monoisotopic mass
189.048954601
InChI
InChI=1S/C6H12N3PS/c11-10(7-1-2-7,8-3-4-8)9-5-6-9/h1-6H2
InChI Key
InChIKey=FOCVUCIESVLUNU-UHFFFAOYSA-N
IUPAC Name
tris(aziridin-1-yl)-$l^{5}-phosphanethione
Traditional IUPAC Name
thiotepa
SMILES
S=P(N1CC1)(N1CC1)N1CC1
Độ tan chảy
51.5 °C
Độ hòa tan
1.9E+005 mg/L (at 25 °C)
logP
0.53
logS
-1.3
pKa (Strongest Basic)
-0.3
PSA
9.03 Å2
Refractivity
50.72 m3·mol-1
Polarizability
18.3 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Dược Lực Học : The unstable nitrogen-carbon groups alkylate with DNA causing irrepairable DNA damage. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Cơ Chế Tác Dụng : N,N'N'-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. It is a stable derivative of N,N',N''- triethylenephosphoramide (TEPA). It is mostly used to treat breast cancer, ovarian cancer and bladder cancer. It is also used as conditioning for Bone marrow transplantation. Its main toxicity is myelosuppression. The alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Dược Động Học :

▧ Route of Elimination :
Urinary excretion of 14C-labeled thiotepa and metabolites in a 34-year old patient with metastatic carcinoma of the cecum who received a dose of 0.3 mg/kg intravenously was 63%.
▧ Half Life :
1.5 to 4.1 hours
▧ Clearance :
* 446 +/- 63 mL/min [female patients (45 to 84 years) with advanced stage ovarian cancer receiving 60 mg and 80 mg thiotepa by intravenous infusion on subsequent courses given at 4-week intervals]
Chỉ Định : ThioTEPA is used a as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients. Also, when high dose chemotherapy with HPCT support it is appropriate for the treatment of solid tumours in adult and paediatric patients.
Tương Tác Thuốc :
  • Bendamustine Increases toxicity through pharmacodynamic synergism. Additive myelosuppression.
  • Bupropion Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Bupropion, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Bupropion if Thiotepa is initiated, discontinued or dose changed.
  • Cyclophosphamide Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Cyclophosphamide, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Cyclophosphamide if Thiotepa is initiated, discontinued or dose changed.
  • Fosphenytoin Possible increase in thiotepa levels
  • Irinotecan Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Irinotecan, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Irinotecan if Thiotepa is initiated, discontinued or dose changed.
  • Ketamine Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Ketamine, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Ketamine if Thiotepa is initiated, discontinued or dose changed.
  • Natalizumab The immunosuppressant, Thiotepa, may increase the adverse effects of Natalizumab. Increased risk of Progressive Multifocal Leukoencephalopathy (PML) and other infections. Concurrent therapy should be avoided.
  • Phenytoin Possible increase in thiotepa levels
  • Promethazine Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Promethazine, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Promethazine if Thiotepa is initiated, discontinued or dose changed.
  • Selegiline Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Selegiline, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Selegiline if Thiotepa is initiated, discontinued or dose changed.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Thiotepa 15 mg vial
    Giá bán buôn : USD >69.6
    Đơn vị tính : vial
  • Biệt dược thương mại : Thiotepa 30 mg vial
    Giá bán buôn : USD >285.0
    Đơn vị tính : vial
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04572
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07641
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00583
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55390-030-10
PharmGKB
http://www.pharmgkb.org/drug/PA451668
Wikipedia
http://en.wikipedia.org/wiki/Thiotepa
RxList
http://www.rxlist.com/thiotepa-drug.htm
Drugs.com
http://www.drugs.com/cdi/thiotepa.html
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