Calcitonin
Calcitonin
Overview
Calcitonin is a 32-amino-acid peptide hormone produced by parafollicular C-cells of the thyroid gland that regulates calcium homeostasis and bone metabolism. Salmon calcitonin (salcatonin) is FDA-approved for treatment of osteoporosis Paget's disease and hypercalcemia and has been used clinically for decades. Calcitonin has a well-established clinical evidence base from its bone disease applications and is additionally studied for analgesic effects in bone pain and as a reference compound for understanding bone mineral metabolism.
Mechanism of Action
Calcitonin acts through the calcitonin receptor (CTR) a G-protein-coupled receptor expressed primarily on osteoclasts — the bone-resorbing cells. CTR activation rapidly inhibits osteoclast activity reducing bone resorption and lowering blood calcium. In the kidneys calcitonin increases calcium and phosphate excretion further reducing serum calcium. The net effect is protection against hypercalcemia and prevention of excessive bone resorption. Salmon calcitonin is approximately 40-50 times more potent than human calcitonin at the receptor due to structural differences and is the form used therapeutically. Beyond calcium regulation calcitonin has central analgesic effects particularly for bone pain — mediated through calcitonin receptors in the central nervous system and modulation of endorphin systems — that are independent of its effects on bone metabolism.
Where does Calcitonin sit?
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Dosage Information
Typical Dose
100-200 IU daily (osteoporosis), 4 IU/kg every 12 hours (hypercalcemia)
Frequency
Daily or every other day depending on indication
Administration
Subcutaneous or intramuscular injection, or intranasal spray (Miacalcin)
Notes
Intranasal formulation is most commonly used for osteoporosis — 200 IU daily alternating nostrils. Injectable forms used for acute hypercalcemia. Resistance can develop with long-term use due to receptor downregulation.
Compound Data
Molecular Formula
C151H226N40O45S3
Molecular Weight
3417.90 g/mol
IUPAC Name
(3S)-4-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-5-amino-1-[[(2S,3R)-1-[[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-5-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(4R,10S,13S,16S,22R)-22-amino-16-(2-amino-2-oxoethyl)-7-[(1R)-1-hydroxyethyl]-10-(hydroxymethyl)-13-(2-methylpropyl)-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexazacyclotricosane-4-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoic acid
PubChem CID
118984394Potential Side Effects
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Quick Facts
- Administration
- Subcutaneous or intramuscular injection, or intranasal spray (Miacalcin)
- Typical Dose
- 100-200 IU daily (osteoporosis), 4 IU/kg every 12 hours (hypercalcemia)
- Frequency
- Daily or every other day depending on indication
- References
- 0 curated + 41 from PubMed
- Clinical Trials
- 49 registered
- Evidence Score
- 70.2 / 100