52232-67-4
52232-67-4 結構式
基本信息
醋酸立特帕肽
特立帕肽
立特帕肽(TERIPARATIDE)
[CYS5,28] PTH (1-34), HUMAN
H-SER-VAL-SER-GLU-ILE-GLN-LEU-MET-HIS-ASN-LEU-GLY-LYS-HIS-LEU-ASN-SER-MET-GLU-ARG-VAL-GLU-TRP-LEU-ARG-LYS-LYS-LEU-GLN-ASP-VAL-HIS-ASN-PHE-OH
PARATHYROID HORMONE (1-34), HUMAN
PARATHYROID HORMONE (HUMAN, 1-34)
PARATHYROID HORMONE HUMAN: FRAGMENT 1-34
PTH (1-34) (HUMAN)
PTH (HUMAN, 1-34)
SER-VAL-SER-GLU-ILE-GLN-LEU-MET-HIS-ASN-LEU-GLY-LYS-HIS-LEU-ASN-SER-MET-GLU-ARG-VAL-GLU-TRP-LEU-ARG-LYS-LYS-LEU-GLN-ASP-VAL-HIS-ASN-PHE
SER-VAL-SER-GLU-ILE-GLN-LEU-MET-HIS-ASN-LEU-GLY-LYS-HIS-LEU-ASN-SER-MET-GLU-ARG-VAL-GLU-TRP-LEU-ARG-LYS-LYS-LEU-GLN-ASP-VAL-HIS-ASN-PHE HUMAN
SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF
TERIPARATIDE
Teriparatide acetate
Pth(1-34)(human) Acetate
PARATHYROID HORMONE FRAGMENT HUMAN 1-34 APPROX. 95%
PARATHYROID HORMONE FRAGMENT HUMAN 1-34 90-95%
Teriparatide, Parathyroid Hormone(1-34),human
parathyroid hormone fragment 1-34 human
PARATHYROID HORMONE (PTH) HUMAN 1-34, MIN 95%
(1-34)-HUMAN PARATHYROID HORMONE
物理化學性質
常見問題列表
特立帕肽皮下注射后吸收及消除速度都很快，皮下注射本品20 μg，達峰時間(tmax)為30 min，半衰期(t1/2 )為60 min，靜脈注射血清半衰期為5 min，絕對生物利用度95%。90%藥物經腎臟清除。
醋酸特立帕肽常見不良反應包括頭暈、背痛、惡心和下肢痙攣等，多為一過性；少見的不良反應包括心律失常、耳聾等。目前認為不良反應發(fā)生與患者年齡和給藥劑量之間無明顯關系。
醋酸特立帕肽可通過抑制成骨細胞凋亡、激活骨襯細胞和增強成骨細胞分化來介導骨代謝。通過調節(jié)腺苷酸環(huán)化酶-環(huán)磷酸腺苷-蛋白激酶A傳導通路間歇性刺激成骨細胞、骨襯細胞和骨髓基質干細胞表面PHT-Ⅰ受體，促進成骨細胞的分化、延長成骨細胞壽命；通過磷酸酯C-胞漿鈣離子-蛋白激酶C信號傳導通路，刺激成骨細胞系增殖；通過抑制PPARγ的反式激活活性，減少基質細胞向脂肪細胞系分化，使成骨細胞數量增加；通過調節(jié)細胞因子間接調節(jié)骨的成長，例如可以誘導iGF-1與成骨細胞結合，從而促進骨的形成；通過Wnt信號通路調節(jié)骨形成的過程，從而增加骨的形成。
2011年復泰奧（特立帕肽）在全球銷售額達到9.51億美元。在中國市場，2011 年由禮來（法國）公司開始進口。
IC50: 2 nM (PTH).
Trabecular bone calcium and dry weight of the distal femur increased significantly in Teriparatide-treated animals. The increase in trabecular calcium compared with vehicle control occurred as early as 1 week after initiation of treatment with a 35% and 45% increase, respectively, for 10 μg/kg and 40 μg/kg Teriparatide. Similar results were observed for trabecular dry weight. After 4 weeks of treatment with 10 mg/kg or 40 mg/kg Teriparatide, trabecular calcium increased significantly by 70% and 123%, respectively, compared with the vehicle and by 73%.
The 4-week Teriparatide administration increase the pore ratio, number, and density as well as the cortical area, thickness, and bone mineral content (BMC), without significant influencing the volumetric bone mineral density (BMD). The 4-week Teriparatide administration + 8-week vehicle administration decrease the pore ratio, number, and density as well as the cortical area and thickness, compared with the 4-week Teriparatide administration, but the pore ratio, cortical area, and thickness are still higher compared with the 12-week vehicle administration. The 4-week Teriparatide administration + 8-week higherdose IBN administration increase the cortical area, thickness, BMC, and volumetric
BMD and decrease the pore ratio, but not the pore number or density, compared with the 4-week Teriparatide administration + 8-week vehicle administration.