Sitaxentan
Các tên gọi khác (3) :
- Sitaxentan
- Sitaxsentan
- Thelin
Thuốc Gốc
Small Molecule
CAS: 210421-64-0
ATC: C02KX03
CTHH: C18H15ClN2O6S2
PTK: 454.905
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
454.905
Monoisotopic mass
454.006005309
InChI
InChI=1S/C18H15ClN2O6S2/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18/h3-5,7,21H,6,8H2,1-2H3
InChI Key
InChIKey=PHWXUGHIIBDVKD-UHFFFAOYSA-N
IUPAC Name
N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2H-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide
Traditional IUPAC Name
sitaxentan
SMILES
CC1=NOC(NS(=O)(=O)C2=C(SC=C2)C(=O)CC2=CC3=C(OCO3)C=C2C)=C1Cl
Độ hòa tan
1.81e-02 g/l
logP
3.09
logS
-4.4
pKa (strongest acidic)
6.89
pKa (Strongest Basic)
0.75
PSA
107.73 Å2
Refractivity
105.8 m3·mol-1
Polarizability
43.12 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học :
Cơ Chế Tác Dụng :
Dược Động Học :
70-100%
▧ Protein binding :
99% +
▧ Metabolism :
Hepatic (CYP2C9- and CYP3A4-mediated)
▧ Route of Elimination :
Renal (50 to 60%) Fecal (40 to 50%)
▧ Half Life :
10 hours
Chỉ Định :
Tương Tác Thuốc :
- Carisoprodol Strong CYP2C19 inhibitors such as sitaxentan may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
- Tamoxifen Sitaxsentan may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sitaxsentan is initiated, discontinued or dose changed.
- Tamsulosin Sitaxsentan, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Sitaxsentan is initiated, discontinued, or dose changed.
- Tofacitinib Sitaxentan (moderate CYP3A4 inhibitors, strong CYP2C19 inhbitors), when used in combination with tofacitinib, may increase tofaciitinib serum concentration toxicity and adverse effects. It is recommended to adjust therapy by reducing the adult dose of tofacitinib from 5mg twice a day to 5 mg daily.
- Tolbutamide Sitaxsentan, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Sitaxsentan is initiated, discontinued or dose changed.
- Tolterodine Sitaxsentan may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
- Torasemide Sitaxsentan, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Sitaxsentan is initiated, discontinued or dose changed.
- Tramadol Sitaxsentan may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance.
- Trazodone The CYP3A4 inhibitor, Sitaxsenten, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Norfloxacin is initiated, discontinued or dose changed.
- Trimethoprim The strong CYP2C9 inhibitor, Sitaxsentan, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Sitaxsentan is initiated, discontinued or dose changed.
- Trimipramine The strong CYP2C19 inhibitor, Sitaxsentan, may decrease the metabolism and clearance of Trimipramine, a CYP2D6 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Sitaxsentan is initiated, discontinued or dose changed.
- Voriconazole Sitaxsentan, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole if sitaxsentan is initiated, discontinued or dose changed.
- Warfarin Sitaxentan, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. Warfarin doses should be decreased by 80% upon initiated of concomitant therapy. Monitor for changes in the therapeutic and adverse effects of warfarin if sitaxentan is initiated, discontinued or dose changed.
- Zafirlukast Sitaxentan, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of zafirlukast. Consider alternate therapy or monitor for changes in zafirlukast therapeutic and adverse effects if sitaxentan is initiated, discontinued or dose changed.
Dữ Kiện Thương Mại
Nhà Sản Xuất
-
Công ty : PfizerSản phẩm biệt dược : Thelin
Tài Liệu Tham Khảo Thêm
drugbank
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PubChem Substance
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