Tìm theo
Teduglutide
Các tên gọi khác (10 ) :
  • (Gly2)glp-2
  • ALX 0600
  • ALX-0600
  • Gattex
  • Glucagon-like peptide ii (2-glycine) (human)
  • Gly(2)-glp-2
  • HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
  • His-gly-asp-gly-ser-phe-ser-asp-glu-met-asn-thr-ile-leu-asp-asn-leu-ala-ala-arg-asp-phe-ile-asn-trp-leu-ile-gln-thr-lys-ile-thr-asp
  • Teduglutide [rDNA origin]
  • Teduglutide Recombinant
Thuốc Gốc
Biotech
CAS: 197922-42-2
ATC: A16AX08
CTHH: C164H252N44O55S
PTK: 3752 Da
Teduglutide is a glucagon-like peptide-2 (GLP-2) analogue. It is made up of 33 amino acids and is manufactured using a strain of Escherichia coli modified by recombinant DNA technology. Teduglutide differs from GLP-2 by one amino acid (alanine is substituted by glycine). The significance of this substitution is that teduglutide is longer acting than endogenous GLP-2 as it is more resistant to proteolysis from dipeptidyl peptidase-4. FDA approved on December 21, 2012.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C164H252N44O55S
Phân tử khối
3752 Da
Dược Lực Học : An enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Teduglutide does not prolong the QTc interval.
Cơ Chế Tác Dụng : Teduglutide is a glucagon-like peptide-2 (GLP-2) analogue. It is made up of 33 amino acids and is manufactured using a strain of Escherichia coli modified by recombinant DNA technology. Teduglutide differs from GLP-2 by one amino acid (alanine is substituted by glycine). The significance of this substitution is that teduglutide is longer acting than endogenous GLP-2 as it is more resistant to proteolysis from dipeptidyl peptidase-4. FDA approved on December 21, 2012. Teduglutide is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
Dược Động Học :
▧ Absorption :
The pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics. Absolute bioavailability, SubQ = 88%; Tmax, SubQ = 3-5 hours; Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL; AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg•hr/mL; Teduglutide does not accumulate following multiple subcutaneous administrations.
▧ Volume of Distribution :
Vd, healthy subjects = 103 mL/kg
▧ Metabolism :
Although a formal investigation has not been conducted, it is expected because teduglutide is a peptide-based drug, it will be degraded into smaller peptides and amino acids via catabolic pathways. The cytochrome P450 enzyme system is not involved in the metabolism of this drug.
▧ Route of Elimination :
Urine
▧ Half Life :
Terminal half-life, healthy subjects = 2 hours; Terminal half-life, SBS patients = 1.3 hours
▧ Clearance :
Plasma clearance, healthy subjects = 123 mL/hr/kg; This value indicates that teduglutide is primarily cleared by the kidney.
Độc Tính : The most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
Chỉ Định : Treatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
Liều Lượng & Cách Dùng : Injection, powder, for solution - Subcutaneous - 5 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Sản phẩm biệt dược : Gattex
  • Công ty :
    Sản phẩm biệt dược : Revestive
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08900
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C16049
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06053
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/68875-0101-2
Wikipedia
http://en.wikipedia.org/wiki/Teduglutide
RxList
http://www.rxlist.com/gattex-drug.htm
Drugs.com
http://www.drugs.com/mtm/teduglutide.html
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