52232-67-4
52232-67-4 結(jié)構(gòu)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(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)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(dá)峰時(shí)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(duì)生物利用度95%。90%藥物經(jīng)腎臟清除。
特立帕肽注射后常見(jiàn)不良反應(yīng)包括頭暈、背痛、惡心和下肢痙攣等，多為一過(guò)性；少見(jiàn)的不良反應(yīng)包括心律失常、耳聾等。目前認(rèn)為不良反應(yīng)發(fā)生與患者年齡和給藥劑量之間無(wú)明顯關(guān)系。
2011年復(fù)泰奧（特立帕肽）在全球銷售額達(dá)到9.51億美元。在中國(guó)市場(chǎng)，2011 年由禮來(lái)（法國(guó)）公司開(kāi)始進(jìn)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.