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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
Systemic clearance of teriparatide (approximately 62 L/hr in women and 94 L/hr in men) exceeds the rate of normal liver plasma flow, consistent with both hepatic and extra-hepatic clearance. Volume of distribution, following intravenous injection, is approximately 0.12 L/kg. Intersubject variability in systemic clearance and volume of distribution is 25% to 50%. Teriparatide is extensively absorbed after subcutaneous injection; the absolute bioavailability is approximately 95% based on pooled data from 20-, 40-, and 80-ug doses. The rates of absorption and elimination are rapid. The peptide reaches peak serum concentrations about 30 minutes after subcutaneous injection of a 20-ug dose and declines to non-quantifiable concentrations within 3 hours. Biological Half-Life The half-life of teriparatide in serum is 5 minutes when administered by intravenous injection and approximately 1 hour when administered by subcutaneous injection. The longer half-life following subcutaneous administration reflects the time required for absorption from the injection site. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation One infant with congenital hyperparathyroidism was breastfed during maternal use of teriparatide. The infant appeared to be protected against hypoparathyroidism by breastfeeding. Monitor breastfed infants for signs and symptoms of hypercalcemia or hypocalcemia. Monitoring of serum calcium monitoring should be considered. Because of the potential for osteosarcoma in animal studies, the manufacturer advises that breastfeeding is not recommended during treatment with teriparatide. ◉ Effects in Breastfed Infants A woman with autosomal dominant hypoparathyroidism type 1 (ADH1) was treated with teriparatide 28 mcg daily by continuous infusion during pregnancy. She also took vitamin D3 1000 IU daily, magnesium oxide 400 mg twice daily, and calcium carbonate 0 to 3 grams orally depending on serum calcium. The infusion was continued for 8 months postpartum in doses ranging from 27 to 30 mcg daily when calcitriol 0.5 mcg twice daily was substituted. She breastfed her infant exclusively for 6 months then with supplementation to 1 year. Her infant had no change in serum calcium when maternal calcitriol was begun. The mother began weaning at 11 months and at 1 year of age when weaning was complete, her infant developed hypocalcemia and was diagnosed with ADH1 and the same genetic mutation as her mother and other family members. Serum parathyroid hormone-related protein levels in the infant were in the mid-normal range during the first year while nursing. A single sample drawn after weaning showed her level had dropped markedly. The breastfed infant appeared to be protected from severe hypocalcemia during the first year of life by the mother’s breastmilk. Growth and development were normal at 1.5 years of age. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Teriparatide can cause cancer according to state or federal government labeling requirements.
Teriparatide is a polypeptide. 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. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995) See also: Teriparatide (annotation moved to). Mechanism of Action The skeletal effects of teriparatide depend upon the pattern of systemic exposure. Once-daily administration of teriparatide stimulates new bone formation on trabecular and cortical (periosteal and/or endosteal) bone surfaces by preferential stimulation of osteoblastic activity over osteoclastic activity. In monkey studies, teriparatide improved trabecular microarchitecture and increased bone mass and strength by stimulating new bone formation in both cancellous and cortical bone. In humans, the anabolic effects of teriparatide are manifest as an increase in skeletal mass, an increase in markers of bone formation and resorption, and an increase in bone strength. By contrast, continuous excess of endogenous PTH, as occurs in hyperparathyroidism, may be detrimental to the skeleton because bone resorption may be stimulated more than bone formation. Endogenous 84-amino-acid parathyroid hormone (PTH) is the primary regulator of calcium and phosphate metabolism in bone and kidney. Physiological actions of PTH include regulation of bone metabolism, renal tubular reabsorption of calcium and phosphate, and intestinal calcium absorption. The biological actions of PTH and teriparatide are mediated through binding to specific high-affinity cell-surface receptors. Teriparatide and the 34 N-terminal amino acids of PTH bind to these receptors with the same affinity and have the same physiological actions on bone and kidney. Teriparatide is not expected to accumulate in bone or other tissues. |
| 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
|
| 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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