Tìm theo
Pomalidomide
Thuốc giảm miễn dịch
Thuốc Gốc
Small Molecule
CAS: 19171-19-8
CTHH: C13H11N3O4
PTK: 273.2441
Pomalidomide, an analogue of thalidomide, is an immunomodulatory antineoplastic agent. FDA approved on February 8, 2013.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H11N3O4
Phân tử khối
273.2441
Monoisotopic mass
273.074955855
InChI
InChI=1/C13H11N3O4/c14-7-3-1-2-6-10(7)13(20)16(12(6)19)8-4-5-9(17)15-11(8)18/h1-3,8H,4-5,14H2,(H,15,17,18)
InChI Key
InChIKey=UVSMNLNDYGZFPF-UHFFFAOYNA-N
IUPAC Name
4-amino-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
Traditional IUPAC Name
pomalidomide
SMILES
NC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O
Độ hòa tan
2.57e+00 g/l
logP
-0.16
logS
-2
pKa (strongest acidic)
11.59
pKa (Strongest Basic)
1.56
PSA
109.57 Å2
Refractivity
69.03 m3·mol-1
Polarizability
25.81 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pomalidomide is more potent than thalidomide (100-times) and lenalidomide (10-times).
Cơ Chế Tác Dụng : Pomalidomide, an analogue of thalidomide, is an immunomodulatory antineoplastic agent. FDA approved on February 8, 2013. Promalidomide is an immunomodulatory agent with antineoplastic activity. It is shown to inhibit the proliferation and induce apoptosis of various tumour cells. Furthermore, promalidomide enhances T cell and natural killer (NK) cell-mediated immunity and inhibited the production of pro-inflammatory cytokines, like TNF-alpha or IL-6, by monocytes. The primary target of promalidomide is thought to be the protein cereblon. It binds to this target and inhibits ubiquitin ligase activity. It is also a transcriptional inhibitor of COX2.
Dược Động Học :
▧ Absorption :
Pomalidomide is generally well absorbed. The major circulating component is the parent compound. Tmax, single oral dose = 2 -3 hours. When 4 mg of promalidomide is given to patients with multiple myeloma, the steady-state pharmacokinetic parameters are as follows: AUC(T) = 400 ng.hr/mL; Cmax = 75 ng/mL. Promalidomide accumulates following multiple doses.
▧ Volume of Distribution :
Mean apparent volume of distribution (Vd/F), steady-state = 62 - 138 L
▧ Protein binding :
12-44% protein bound. It is not concentration dependent.
▧ Metabolism :
Promalidomide is hepatically metabolized by CYP1A2 and CYP3A4. The metabolites are 26-fold less active than the parent compound. Minor contributions from CYP2C19 and CYP2D6 have been observed in vitro.
▧ Route of Elimination :
When a single oral dose (2mg) is given to healthy subjects, 73% of the dose was eliminated in urine. 15% of the dose was eliminated in feces. 2% and 8% of the dose eliminated unchanged as pomalidomide in urine and feces, respectively.
▧ Half Life :
Healthy subjects = 9.4 hours; Multiple myeloma patients = 7.5 hours.
▧ Clearance :
Total body clearance = 7-10 L/hour
Độc Tính : Most common adverse reactions (≥30%) included fatigue and asthenia, neutropenia, anemia, constipation, nausea, diarrhea, dyspnea, upper-respiratory tract infections, back pain and pyrexia.
Chỉ Định : Pomalidomide is indicated for patients with multiple myeloma who have received at least two prior therapies including lenalidomide and bortezomib and have demonstrated disease progression on or within 60 days of completion of the last therapy.
Tương Tác Thuốc :
  • Ketoconazole Strong CYP3A4 inhibitors may increase levels of pomalidomide. Concomitant therapy should be avoided.
  • Rifampicin Strong CYP3A4 inducers may decrease levels of pomalidomide. Concomitant therapy should be avoided.
Liều Lượng & Cách Dùng : Capsule - Oral - 1 mg, 2 mg, 3 mg, 4 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Imnovid
  • Công ty : Celgene
    Sản phẩm biệt dược : Pomalyst
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08910
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08976
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59572-504-21
Wikipedia
http://en.wikipedia.org/wiki/Pomalidomide
RxList
http://www.rxlist.com/pomalyst-drug.htm
Drugs.com
http://www.drugs.com/cdi/pomalidomide.html
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