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Teriparatide (HSDB 7367; ZT034; Human parathyroid hormone 1-34; trade name Forteo), a recombinant form of parathyroid hormone (consisting of the first 34 amino acids of PHT), is a potent parathyroid hormone (PTH) agonist that has been approved in 2017 as an anabolic agent for the treatment of some forms of osteoporosis. As a PHT agonist, it inhibits PHT with an IC50 of 2 nM in HEK293 cells.
| Targets |
PTH (IC50 = 2 nM)[1]
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|---|---|
| ln Vitro |
Teriparatide is a polypeptide that acts as a PTH1 receptor agonist. It can also cause cancer according to state or federal government labeling requirements. It is a polypeptide that consists of the 1-34 amino-acid fragment of human PARATHYROID HORMONE, the biologically active N-terminal region. The acetate form is given by intravenous infusion in the differential diagnosis of HYPOPARATHYROIDISM and PSEUDOHYPOPARATHYROIDISM.
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| ln Vivo |
Teriparatide (human parathyroid hormone-(1-34)) (20 μg/kg ih; once daily for 4 weeks; female New Zealand White rabbits) increases body weight and obesity [1].
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| Animal Protocol |
Animal/Disease Models: Female New Zealand White rabbit [1]
Doses: 20 μg/kg Route of Administration: subcutaneous injection; one time/day for 4 weeks Experimental Results: Increased porosity, number and density as well as cortical area, thickness and bone mineral content (BMC), but had no significant effect on volumetric bone mineral density (BMD). Forty-two female New Zealand white rabbits (17–21 weeks old) were housed in an animal room (temperature, 19 °C; humidity, 50 %; and a 12-h on/off light cycle) with free access to water. Rabbits were fed a chow diet (RC-4, 120 g/day). After 10 days of adaptation to their new environment, the rabbits (18–22 weeks old) were randomized into six groups of 7 animals each using the stratified weight method, as follows: 4-week vehicle administration group (4W-Veh), 4-week Teriparatide (TPTD) administration group (4W-TPTD: 20 μg/kg, subcutaneously [s.c.], daily), 12-week vehicle administration group (12W-Veh), 4-week TPTD administration + 8-week vehicle administration group (4W-TPTD + 8W-Veh), 4-week TPTD administration + 8-week lower-dose IBN administration group (4W-TPTD + 8W-IBN(L): 20 μg/kg of IBN, s.c., every 4 weeks), and 4-week TPTD administration + 8-week higher-dose IBN administration group (4W-TPTD + 8W-IBN(H): 100 μg/kg of IBN, s.c., every 4 weeks). The TPTD (human recombinant teriparatide) dose was selected based on the results of a previous rabbit study. The IBN doses were determined based on the results of previous ovariectomized monkey studies. Body weight was monitored weekly.[1] |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Teriparatide's systemic clearance (approximately 62 L/hr for women and 94 L/hr for men) exceeds normal hepatic plasma flow, consistent with both hepatic and extrahepatic clearance. Following intravenous injection, the volume of distribution is approximately 0.12 L/kg. Inter-individual variability in systemic clearance and volume of distribution ranges from 25% to 50%. Following subcutaneous injection, teriparatide is extensively absorbed; based on pooled data from the 20 μg, 40 μg, and 80 μg dose groups, its absolute bioavailability is approximately 95%. Both absorption and elimination rates are rapid. Following a 20 μg subcutaneous dose, serum concentrations of the peptide peak within approximately 30 minutes and decline to undetectable levels within 3 hours. Biological Half-Life The serum half-life of teriparatide after intravenous injection is 5 minutes, and after subcutaneous injection, it is approximately 1 hour. A longer half-life after subcutaneous injection reflects the time required for the drug to be absorbed from the injection site. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation An infant with congenital hyperparathyroidism was breastfed while the mother was using teriparatide. Breastfeeding appeared to protect the infant from the effects of hypoparathyroidism. Signs and symptoms of hypercalcemia or hypocalcemia should be monitored in breastfed infants. Monitoring of serum calcium levels should be considered. Due to the potential risk of osteosarcoma identified in animal studies, the manufacturer recommends against breastfeeding during teriparatide treatment. ◉ Effects on Breastfed Infants A woman with autosomal dominant hypoparathyroidism type 1 (ADH1) received teriparatide treatment during pregnancy at 28 mcg daily via continuous intravenous infusion. She also took 1000 IU of vitamin D3 daily, 400 mg of magnesium oxide twice daily, and 0 to 3 g of calcium carbonate orally based on serum calcium levels. Eight months postpartum, the mother continued calcitriol infusions at a dose of 27 to 30 micrograms daily, then reduced to 0.5 micrograms twice daily. The mother exclusively breastfed the infant for six months, followed by complementary feeding until one year of age. The infant's serum calcium levels did not change after the mother began calcitriol administration. The mother began weaning the infant at 11 months of age. After weaning, the infant developed hypocalcemia and was diagnosed with ADH1, sharing the same gene mutation as the mother and other family members. During the first year of lactation, the infant's serum parathyroid hormone-related protein levels were within the median of the normal range. A sample collected after weaning showed a significant decrease in these levels. Breastfed infants appear to be protected from severe hypocalcemia by their mother's milk during the first year of life. Growth and development were normal at 1.5 years of age. ◉ Effects on Lactation and Breast Milk No relevant published information was found as of the revision date. |
| References | |
| Additional Infomation |
Teriparatide may be carcinogenic, depending on state or federal labeling requirements. Teriparatide is a polypeptide. This polypeptide consists of a 1-34 amino acid segment of human parathyroid hormone, specifically the biologically active N-terminal region. The acetate form is used for the differential diagnosis of hypoparathyroidism and pseudohypoparathyroidism and can be administered via intravenous infusion. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995) See also: Teriparatide (note moved to). Mechanism of Action: The effects of teriparatide on bone depend on the pattern of systemic exposure. Once-daily injections of teriparatide promote new bone formation on the surface of cancellous and cortical bone (periosteum and/or endosteum) by preferentially stimulating osteoblast activity rather than osteoclast activity. In monkey studies, teriparatide improved trabecular microstructure and increased bone mass and strength by stimulating new bone formation in cancellous and cortical bone. In humans, the anabolic effects of teriparatide manifest as increased bone mass, elevated markers of bone formation and resorption, and enhanced bone strength. Conversely, persistent excesses of endogenous parathyroid hormone (PTH) (such as in hyperparathyroidism) can be detrimental to bone because bone resorption may be stimulated more than bone formation. Endogenous parathyroid hormone (PTH), composed of 84 amino acids, is a major regulator of calcium and phosphorus metabolism in bone and kidneys. The physiological functions of PTH include regulating bone metabolism, renal tubular reabsorption of calcium and phosphate, and intestinal calcium absorption. The biological effects of PTH and teriparatide are mediated by binding to specific high-affinity cell surface receptors. The 34 N-terminal amino acids of teriparatide and PTH bind to these receptors with the same affinity and produce the same physiological effects on bone and kidneys. Teriparatide is not expected to accumulate in bone or other tissues.
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| Molecular Formula |
C181H291N55O51S2.C2H4O2
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|---|---|
| Molecular Weight |
4177.77
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| Exact Mass |
4116.134
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| Elemental Analysis |
C, 52.80; H, 7.12; N, 18.71; O, 19.82; S, 1.56
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| CAS # |
52232-67-4
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| Related CAS # |
Teriparatide acetate hydrate;99294-94-7
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| PubChem CID |
16133850
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| Sequence |
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;
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; L-seryl-L-valyl-L-seryl-L-alpha-glutamyl-L-isoleucyl-L-glutaminyl-L-leucyl-L-methionyl-L-histidyl-L-asparagyl-L-leucyl-glycyl-L-lysyl-L-histidyl-L-leucyl-L-asparagyl-L-seryl-L-methionyl-L-alpha-glutamyl-L-arginyl-L-valyl-L-alpha-glutamyl-L-tryptophyl-L-leucyl-L-arginyl-L-lysyl-L-lysyl-L-leucyl-L-glutaminyl-L-alpha-aspartyl-L-valyl-L-histidyl-L-asparagyl-L-phenylalanine |
| SequenceShortening |
SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF
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| Appearance |
White to off-white solid powder
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| LogP |
-18.7
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| Hydrogen Bond Donor Count |
60
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| Hydrogen Bond Acceptor Count |
62
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| Rotatable Bond Count |
146
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| Heavy Atom Count |
289
|
| Complexity |
9740
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| Defined Atom Stereocenter Count |
34
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| SMILES |
[SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF]
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| InChi Key |
OGBMKVWORPGQRR-UMXFMPSGSA-N
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| InChi Code |
InChI=1S/C181H291N55O51S2/c1-21-96(18)146(236-160(267)114(48-53-141(250)251)212-174(281)132(84-239)232-177(284)143(93(12)13)233-147(254)103(185)82-237)178(285)216-111(45-50-134(187)241)155(262)219-119(65-90(6)7)163(270)213-116(55-62-289-20)158(265)224-124(71-100-79-196-86-203-100)167(274)226-126(73-135(188)242)169(276)217-117(63-88(2)3)148(255)201-81-138(245)205-105(39-27-30-56-182)149(256)223-123(70-99-78-195-85-202-99)166(273)221-121(67-92(10)11)164(271)225-128(75-137(190)244)171(278)231-131(83-238)173(280)214-115(54-61-288-19)157(264)210-112(46-51-139(246)247)153(260)208-109(43-34-60-199-181(193)194)159(266)234-144(94(14)15)175(282)215-113(47-52-140(248)249)156(263)222-122(69-98-77-200-104-38-26-25-37-102(98)104)165(272)220-120(66-91(8)9)161(268)209-108(42-33-59-198-180(191)192)151(258)206-106(40-28-31-57-183)150(257)207-107(41-29-32-58-184)152(259)218-118(64-89(4)5)162(269)211-110(44-49-133(186)240)154(261)228-129(76-142(252)253)172(279)235-145(95(16)17)176(283)229-125(72-101-80-197-87-204-101)168(275)227-127(74-136(189)243)170(277)230-130(179(286)287)68-97-35-23-22-24-36-97/h22-26,35-38,77-80,85-96,103,105-132,143-146,200,237-239H,21,27-34,39-76,81-84,182-185H2,1-20H3,(H2,186,240)(H2,187,241)(H2,188,242)(H2,189,243)(H2,190,244)(H,195,202)(H,196,203)(H,197,204)(H,201,255)(H,205,245)(H,206,258)(H,207,257)(H,208,260)(H,209,268)(H,210,264)(H,211,269)(H,212,281)(H,213,270)(H,214,280)(H,215,282)(H,216,285)(H,217,276)(H,218,259)(H,219,262)(H,220,272)(H,221,273)(H,222,263)(H,223,256)(H,224,265)(H,225,271)(H,226,274)(H,227,275)(H,228,261)(H,229,283)(H,230,277)(H,231,278)(H,232,284)(H,233,254)(H,234,266)(H,235,279)(H,236,267)(H,246,247)(H,248,249)(H,250,251)(H,252,253)(H,286,287)(H4,191,192,198)(H4,193,194,199)/t96-,103-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,143-,144-,145-,146-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid
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| Synonyms |
PTH 1-34; HSDB7367; ZT 034; HSDB-7367; Parathar; Teriparatide acetate; 52232-67-4; Teriparatida; ZT034; ZT-034; HSDB 7367; Human parathyroid hormone 1-34; trade name Forteo
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~24.29 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (12.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2394 mL | 1.1968 mL | 2.3936 mL | |
| 5 mM | 0.0479 mL | 0.2394 mL | 0.4787 mL | |
| 10 mM | 0.0239 mL | 0.1197 mL | 0.2394 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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