Tìm theo
Fingolimod
Các tên gọi khác (2) :
  • Fingolimodum
  • FTY720
Thuốc Gốc
Small Molecule
CAS: 162359-55-9
ATC: L04AA27
CTHH: C19H33NO2
PTK: 307.4708
Fingolimod is a sphingosine 1-phosphate receptor modulator indicated and approved for the treatment of relapsing-remitting multiple sclerosis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H33NO2
Phân tử khối
307.4708
Monoisotopic mass
307.251129305
InChI
InChI=1S/C19H33NO2/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-22/h9-12,21-22H,2-8,13-16,20H2,1H3
InChI Key
InChIKey=KKGQTZUTZRNORY-UHFFFAOYSA-N
IUPAC Name
2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol
Traditional IUPAC Name
fingolimod
SMILES
CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1
Độ sôi
479.498 °C at 760 mmHg
Độ hòa tan
Soluble
logP
4.178
logS
-4.7
pKa (strongest acidic)
14.41
pKa (Strongest Basic)
9.38
PSA
66.48 Å2
Refractivity
93.28 m3·mol-1
Polarizability
39.03 Å3
Rotatable Bond Count
12
H Bond Acceptor Count
3
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Fingolimod causes a transient reduction in heart rate and AV conduction at treatment initiation. Potential to prolong the QT interval. Effects on immune cell numbers in the blood- decreased lymphocyte counts. Mild decrease in the neutrophil count- about 80% of original pre-therapy count. Compared to placebo, antigen-specific IgM titers were decreased by 91% and 25% in response to KLH and PPV, respectively. IgG titers were decreased by 45% and 50%, in response to KLH and PPV. The capacity to mount a skin delayed-type hypersensitivity reaction to Candida and tetanus toxoid was decreased by approximately 30% in subjects on fingolimod 0.5 mg daily, compared to placebo. Immunologic responses were further decreased with fingolimod 1.25 mg (a dose higher than recommended for MS). Single fingolimod doses ≥5 mg (10-fold the recommended dose) are associated with a dose-dependent increase in airway resistance.
Cơ Chế Tác Dụng : Fingolimod is a sphingosine 1-phosphate receptor modulator indicated and approved for the treatment of relapsing-remitting multiple sclerosis. Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimod-phosphate is a sphingosine 1-phosphate receptor modulator, and binds with high affinity to sphingosine 1-phosphate receptors 1, 3, 4, and 5. Fingolimod-phosphate blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which fingolimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system.
Dược Động Học :
▧ Absorption :
The Tmax of fingolimod is 12-16 hours. Bioavailability: 93%
▧ Volume of Distribution :
about 1200±260 L.
▧ Protein binding :
>99.7%
▧ Metabolism :
3 main pathways: -reversible stereoselective phosphorylation to the pharmacologically active (S)-enantiomer of fingolimod-phosphate. -oxidative biotransformation mainly via the cytochrome P450 4F2 isoenzyme and subsequent fatty acid-like degradation to inactive metabolites. -by formation of pharmacologically inactive non-polar ceramide analogs of fingolimod.
▧ Half Life :
6-9 days
▧ Clearance :
Fingolimod blood clearance is 6.3±2.3 L/h.
Độc Tính : Bradyarrhythmia and Atrioventricular Blocks Risk of infections Macular Edema Respiratory Effects Hepatic Effects Fetal Risk Blood Pressure Effects Immune System Effects Following Fingolimod Discontinuation
Chỉ Định : Fingolimod is a sphingosine 1-phosphate receptor modulator indicated for the treatment of patients with relapsing forms of multiple sclerosis to reduce the frequency of clinical exacerbations and to delay the accumulation of physical disability.
Tương Tác Thuốc :
  • Amiodarone Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Belimumab Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
  • Disopyramide Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Dofetilide Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Dronedarone Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Ibutilide Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Ketoconazole Exposure is increased by 70% during concomitant use with systemic ketoconazole, and risk of adverse reactions is greater.
  • Procainamide Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Quinidine Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Sotalol Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
Liều Lượng & Cách Dùng : Capsule - Oral - 0.5mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08868
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D10001
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0607-51
Wikipedia
http://en.wikipedia.org/wiki/Fingolimod
RxList
http://www.rxlist.com/gilenya-drug.htm
Drugs.com
http://www.drugs.com/cdi/fingolimod.html
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