52232-67-4
52232-67-4 结构式
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
物理化学性质
常见问题列表
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，达峰时间(tmax)为30 min，半衰期(t1/2 )为60 min，静脉注射血清半衰期为5 min，绝对生物利用度95%。90%药物经肾脏清除。
特立帕肽注射后常见不良反应包括头晕、背痛、恶心和下肢痉挛等，多为一过性；少见的不良反应包括心律失常、耳聋等。目前认为不良反应发生与患者年龄和给药剂量之间无明显关系。
2011年复泰奥（特立帕肽）在全球销售额达到9.51亿美元。在中国市场，2011 年由礼来（法国）公司开始进口。
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.