|Legal status||Rx only (US)|
|Metabolism||Hepatic (nonspecific proteolysis)|
|Half-life||SubQ: 1 hour|
|Mol. mass||4117.72 g/mol|
| (what is this?)
Teriparatide is administered by injection once a day in the thigh or abdomen. The recommended dose is 20 μg per day.
Teriparatide is indicated for use in postmenopausal women with osteoporosis at a high risk for fracture or with a history of osteoporotic fracture, patients with multiple risk factors for fracture, and for patients who have failed or are intolerant to other available osteoporosis therapy.
One randomized trial of postmenopausal women who had already fractured vertebra compared teriparatide at either 20 or 40 micrograms per day with placebo. After about 19 months, 14% of the women taking placebo had new vertebral fractures, as compared with 5% of the women taking 20 micrograms of teriparatide and 4% of the women taking 40 micrograms. There were also a statistically significant lower number of non-vertebral fractures in the teriparatide treated group. 20 micrograms of teriparatide increased spine and hip bone mineral density.
Teriparatide is also indicated to increase bone mass in men with primary or hypogonadal osteoporosis at high risk of fracture, patients with multiple risk factors for fracture, and for patients who have failed or are intolerant to other available osteoporosis therapy.
Teriparatide is indicated as well for the treatment of men and women with osteoporosis associated with sustained systemic glucocorticoid therapy.
Teriparatide should not be prescribed for patients who are at increased risks for osteosarcoma. This includes those with Paget's Disease of bone or unexplained elevations of serum alkaline phosphate, open epiphysis, or prior radiation therapy involving the skeleton.
Teriparatide is used as off-label therapy to speed fracture repair and treat fracture nonunions. Generally, due to HIPPA regulations, it is not publicized when American athletes receive this treatment to improve fracture recovery. But an Italian soccer player, Francesco Totti, was given teriparatide after a tibia/fibula fracture, and he unexpectedly recovered in time for the 2006 World Cup. It has been reported that Mark Mulder used it to recover from a hip fracture Oakland A's for the 2003 MLB playoffs and Terrell Owens to recover from an ankle fracture before the 2005 Super Bowl.
Teriparatide has a theoretical risk of osteosarcoma, which was found in rat studies but not confirmed in humans. Unlike humans, rat bones grow for their entire life. The tumors found in the rat studies were located on the end of the bones which grew after the injections began.
Mechanism of action
Teriparatide is a portion of human parathyroid hormone (PTH), amino acid sequence 1 through 34, of the complete molecule (containing 84 amino acids). Endogenous PTH is the primary regulator of calcium and phosphate metabolism in bone and kidney. PTH increases serum calcium, partially accomplishing this by increasing bone resorption. Thus, chronically elevated PTH will deplete bone stores. However, intermittent exposure to PTH will activate osteoblasts more than osteoclasts. Thus, once-daily injections of teriparatide have a net effect of stimulating new bone formation leading to increased bone mineral density.
Teriparatide is the first, and to date only, FDA approved agent for the treatment of osteoporosis that stimulates new bone formation.
Teriparatide was approved by the Food and Drug Administration (FDA) on 26 November 2002, for the treatment of osteoporosis in men and postmenopausal women who are at high risk for having a fracture. The drug is also approved to increase bone mass in men with primary or hypogonadal osteoporosis who are at high risk for fracture.
Combined teriparatide and denosumab
Combined teriparatide and denosumab increased BMD more than either agent alone and more than has been reported with approved therapies. Combination treatment might, therefore, be useful to treat patients at high risk of fracture.
- Saag KG, Shane E, Boonen S, et al. (November 2007). "Teriparatide or alendronate in glucocorticoid-induced osteoporosis". The New England Journal of Medicine 357 (20): 2028–39. doi:10.1056/NEJMoa071408. PMID 18003959.
- N Engl J Med. 2001 May 10;344(19):1434-41.
- Bruce Jancin (2011-12-12). "Accelerating Fracture Healing With Teriparatide". Internal Medicine News Digital Network. Retrieved 2013-09-20.
- William L. Carroll (2005). "Chapter 1: Defining the Issue". The Juice: The Real Story of Baseball's Drug Problems. ISBN 1-56663-668-X. Retrieved 2013-09-23.
- Bauer E, Aub JC, Albright F. Studies of calcium and phosphorus metabolism: V. Study of the bone trabeculae as a readily available reserve supply of calcium. J Exp Med. 1929;49:145-162.
- Selye H. On the stimulation of new bone formation with parathyroid extract and irradiated ergosterol. Endocrinology. 1932;16:547-558.
- Dempster, D.W., Cosman, F., Parisien, M., Shen, V., & R. Lindsay. "Anabolic actions of parathyroid hormone on bone." (1993). Endocrine Review: 14(6): 690-709.
- Fortéo: teriparatide (rDNA origin) injection
- Joy N Tsai MD,Alexander V Uihlein MD,Hang Lee PhD,Ruchit Kumbhani BA,Erica Siwila-Sackman BA,Elizabeth A McKay BA,Sherri-Ann M Burnett-Bowie MD,Robert M Neer MD,Dr Benjamin Z Leder MD. Teriparatide and denosumab, alone or combined, in women with postmenopausal osteoporosis: the DATA study randomised trial. The Lancet - 15 May 2013 DOI: 10.1016/S0140-6736(13)60856-9