Palopegteriparatide is a parathyroid hormone analog used to treat hyperparathyroidism in adults. Palopegteriparatide is a prodrug consisting of PTH(1-34) conjugated to a methoxy polyethylene glycol carrier (mPEG) via a proprietary TransCon Linker.
- Mechanism
- Curator reviewed · 8 references
Secreted by the parathyroid glands, endogenous parathyroid hormone (PTH) is an 84-amino acid-long polypeptide that binds to cell-surface parathyroid hormone receptors expressed in various tissues. The main receptor is parathyroid hormone 1 receptor (PTH1R), which is highly expressed in osteoblasts, osteocytes, renal tubular cells, and several other tissues. PTH maintains extracellular calcium and phosphate homeostasis by increasing serum calcium and decreasing serum phosphate. PTH stimulates bone turnover to mobilize calcium and phosphate from bone, promotes renal calcium reabsorption and phosphate excretion, and facilitates active vitamin D synthesis, in turn increasing intestinal absorption of calcium and phosphate. PTH deficiency due to hypoparathyroidism can lead to low bone turnover and structural and dynamic skeletal defects if not addressed.
Palopegteriparatide is a prodrug that releases PTH(1-34) via autocleavage of the TransCon linker. PTH(1-34) released from palopegteriparatide mimics the biological effects of endogenous PTH.L51124] PTH(1-34) and its active metabolite, PTH(1-33), have similar affinity to and activation of PTH1R as endogenous PTH.
- Primary indication
- Palopegteriparatide is indicated for the treatment of hypoparathyroidism in adults.Curator reviewed · 1 structured indication
- Formula / weight
- 474000.0 Da (approximate)
- First approval
- Canada, 2026 · United States, 2024 · European Union, 2024
- Also known as
- Human parathyroid hormone (PTH) synthetic peptide fragment (1-34), conjugated at the N-terminal amino group via a cleavable linker to O-methylpolyethylene glycol (2 x 20 kDa mPEG); 2-methylalanyl-(1-34)-peptide of parathyroid hormone (Homo sapiens parath · Mpeg 40000-teriparatide · Poly(oxy-1,2-ethanediyl), α-hydro-ω-methoxy-, ether with N-[[[2-[[6-[[1-[3-[[3-(2,3-dihydroxypropoxy)propyl]amino]-3-oxopropyl]-2,5-dioxo-3-pyrrolidinyl]thio]hexyl]amino]ethyl]amino]carbonyl]-2-methylalanyl-L-seryl-L-valyl-L-seryl-L-α-glutamyl-L-isole · Transcon parathyroid hormone (1-34) · TransCon PTH
- Code names
- ACP-014
- Brand names
Resolves to
What you can answer from here — as of August 23, 2024
Which drugs share a target with Palopegteriparatide, and which of those have an active Phase 3 trial?
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