Peringatan Keamanan

There is no information regarding the acute toxicity (LD50) of palopegteriparatide. An accidental overdose of palopegteriparatide may cause hypercalcemia, which can be severe and require medical intervention.L51124 The manifestations of hypercalcemia may include dehydration, heart palpitations, ECG changes, hypotension, nausea, vomiting, dizziness, muscle weakness, and confusion.L51134

One subject in Study 1 accidentally received approximately 3-fold the prescribed dose of palopegteriparatide for more than seven consecutive days and developed albumin-corrected serum calcium as high as 16.1 mg/dL, requiring hospitalization.L51124 After withholding palopegteriparatide, calcium, and active vitamin D, the patient recovered and restarted on the correct dose.L51134

Palopegteriparatide

DB18676

biotech approved investigational

Deskripsi

Palopegteriparatide is a parathyroid hormone (PTH) analog. Palopegteriparatide is a prodrug consisting of PTH(1-34) conjugated to a methoxy polyethylene glycol carrier (mPEG) via a proprietary TransCon Linker.L51134 PTH(1-34) contains the N-terminal part of the endogenous PTH molecule.A264199 Upon administration, PTH is cleaved from palopegteriparatide in a controlled manner to achieve a continuous systemic exposure of active PTH.L51134 Palopegteriparatide was first approved by the EMA on November 17, 2023, for the treatment of hyperparathyroidism.L51134 On August 8, 2024, palopegteriparatide was also approved by the FDA.L51129

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent half-life of PTH released from palopegteriparatide is approximately 60 hours.[L51124]
Volume Distribusi The estimated apparent volume of distribution (CV%) of palopegteriparatide is 4.8 (50) L.[L51124] The apparent volume of distribution (CV%) is 8.7 L (18%) for released PTH.[L51134]
Klirens (Clearance) The estimated clearance (CV%) of palopegteriparatide at steady-state is 0.58 (52) L/day.[L51124]

Absorpsi

PTH Cmax and AUC increased proportionally over a YORVIPATH dosage range of 12 to 24 mcg/day. PTH steady state is achieved after administration of palopegteriparatide for seven days. At steady-state, administration of palopegteriparatide resulted in continuous exposure to released PTH throughout the 24-hour dosing period.L51124 The median (range) time to reach maximum concentrations (Tmax) of PTH is 4 (4-8) hours.L51124

Metabolisme

Released PTH includes PTH(1-34) and the active metabolite PTH(1-33). PTH(1-33) and PTH(1-34) have comparable affinity to and activation of PTH1R.L51124 In the liver, most of the PTH is cleaved by cathepsins.L51134

Rute Eliminasi

PTH is renally metabolized and cleared.L51134 In the kidney, most of PTH is excreted by glomerular filtration.L51134

Interaksi Obat

216 Data
Fluvoxamine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Fluvoxamine.
Citalopram The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Citalopram.
Fluoxetine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Fluoxetine.
Duloxetine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Duloxetine.
Trazodone The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Trazodone.
Paroxetine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Paroxetine.
Sertraline The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Sertraline.
Sibutramine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Sibutramine.
Nefazodone The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Nefazodone.
Escitalopram The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Escitalopram.
Zimelidine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Zimelidine.
Dapoxetine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Dapoxetine.
Milnacipran The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Milnacipran.
Desvenlafaxine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Desvenlafaxine.
Seproxetine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Seproxetine.
Indalpine The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Indalpine.
Ritanserin The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Ritanserin.
Alaproclate The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Alaproclate.
Amphetamine The risk or severity of adverse effects can be increased when Amphetamine is combined with Palopegteriparatide.
Phentermine The risk or severity of adverse effects can be increased when Phentermine is combined with Palopegteriparatide.
Midodrine The risk or severity of adverse effects can be increased when Midodrine is combined with Palopegteriparatide.
Norepinephrine The risk or severity of adverse effects can be increased when Norepinephrine is combined with Palopegteriparatide.
Phenylephrine The risk or severity of adverse effects can be increased when Phenylephrine is combined with Palopegteriparatide.
Phenylpropanolamine The risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Palopegteriparatide.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Palopegteriparatide.
Metaraminol The risk or severity of adverse effects can be increased when Metaraminol is combined with Palopegteriparatide.
Epinephrine The risk or severity of adverse effects can be increased when Epinephrine is combined with Palopegteriparatide.
Methoxamine The risk or severity of adverse effects can be increased when Methoxamine is combined with Palopegteriparatide.
Orciprenaline The risk or severity of adverse effects can be increased when Orciprenaline is combined with Palopegteriparatide.
Phenmetrazine The risk or severity of adverse effects can be increased when Phenmetrazine is combined with Palopegteriparatide.
Dobutamine The risk or severity of adverse effects can be increased when Dobutamine is combined with Palopegteriparatide.
Pseudoephedrine The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with Palopegteriparatide.
Benzphetamine The risk or severity of adverse effects can be increased when Benzphetamine is combined with Palopegteriparatide.
Ritodrine The risk or severity of adverse effects can be increased when Ritodrine is combined with Palopegteriparatide.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Palopegteriparatide.
Oxymetazoline The risk or severity of adverse effects can be increased when Oxymetazoline is combined with Palopegteriparatide.
Diethylpropion The risk or severity of adverse effects can be increased when Diethylpropion is combined with Palopegteriparatide.
Dopamine The risk or severity of adverse effects can be increased when Dopamine is combined with Palopegteriparatide.
Isoprenaline The risk or severity of adverse effects can be increased when Isoprenaline is combined with Palopegteriparatide.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Palopegteriparatide.
Lisdexamfetamine The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with Palopegteriparatide.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Palopegteriparatide.
Ephedrine The risk or severity of adverse effects can be increased when Ephedrine is combined with Palopegteriparatide.
Mephentermine The risk or severity of adverse effects can be increased when Mephentermine is combined with Palopegteriparatide.
Procaterol The risk or severity of adverse effects can be increased when Procaterol is combined with Palopegteriparatide.
Clenbuterol The risk or severity of adverse effects can be increased when Clenbuterol is combined with Palopegteriparatide.
MMDA The risk or severity of adverse effects can be increased when MMDA is combined with Palopegteriparatide.
Midomafetamine The risk or severity of adverse effects can be increased when Midomafetamine is combined with Palopegteriparatide.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Palopegteriparatide.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Palopegteriparatide.
Tenamfetamine The risk or severity of adverse effects can be increased when Tenamfetamine is combined with Palopegteriparatide.
Chlorphentermine The risk or severity of adverse effects can be increased when Chlorphentermine is combined with Palopegteriparatide.
Methylenedioxyethamphetamine The risk or severity of adverse effects can be increased when Methylenedioxyethamphetamine is combined with Palopegteriparatide.
Dextroamphetamine The risk or severity of adverse effects can be increased when Dextroamphetamine is combined with Palopegteriparatide.
Metamfetamine The risk or severity of adverse effects can be increased when Metamfetamine is combined with Palopegteriparatide.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Palopegteriparatide.
Nylidrin The risk or severity of adverse effects can be increased when Nylidrin is combined with Palopegteriparatide.
Levonordefrin The risk or severity of adverse effects can be increased when Levonordefrin is combined with Palopegteriparatide.
Naphazoline The risk or severity of adverse effects can be increased when Naphazoline is combined with Palopegteriparatide.
Tetryzoline The risk or severity of adverse effects can be increased when Tetryzoline is combined with Palopegteriparatide.
Tyramine The risk or severity of adverse effects can be increased when Tyramine is combined with Palopegteriparatide.
Isoxsuprine The risk or severity of adverse effects can be increased when Isoxsuprine is combined with Palopegteriparatide.
Etilefrine The risk or severity of adverse effects can be increased when Etilefrine is combined with Palopegteriparatide.
Synephrine The risk or severity of adverse effects can be increased when Synephrine is combined with Palopegteriparatide.
Iofetamine I-123 The risk or severity of adverse effects can be increased when Iofetamine I-123 is combined with Palopegteriparatide.
Racepinephrine The risk or severity of adverse effects can be increased when Racepinephrine is combined with Palopegteriparatide.
Ritobegron The risk or severity of adverse effects can be increased when Ritobegron is combined with Palopegteriparatide.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with Palopegteriparatide.
Tramazoline The risk or severity of adverse effects can be increased when Tramazoline is combined with Palopegteriparatide.
Mephedrone The risk or severity of adverse effects can be increased when Mephedrone is combined with Palopegteriparatide.
Fenozolone The risk or severity of adverse effects can be increased when Fenozolone is combined with Palopegteriparatide.
Methoxyphenamine The risk or severity of adverse effects can be increased when Methoxyphenamine is combined with Palopegteriparatide.
Tretoquinol The risk or severity of adverse effects can be increased when Tretoquinol is combined with Palopegteriparatide.
Gepefrine The risk or severity of adverse effects can be increased when Gepefrine is combined with Palopegteriparatide.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with Palopegteriparatide.
Prenalterol The risk or severity of adverse effects can be increased when Prenalterol is combined with Palopegteriparatide.
Mefenorex The risk or severity of adverse effects can be increased when Mefenorex is combined with Palopegteriparatide.
2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Palopegteriparatide.
Gefitinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Gefitinib.
Sorafenib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Sorafenib.
Erlotinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Erlotinib.
Imatinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Imatinib.
Dasatinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Dasatinib.
Lapatinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Lapatinib.
Sunitinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Sunitinib.
Genistein The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Genistein.
3-[4-(1-formylpiperazin-4-yl)-benzylidenyl]-2-indolinone The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with 3-[4-(1-formylpiperazin-4-yl)-benzylidenyl]-2-indolinone.
Geldanamycin The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Geldanamycin.
PD173955 The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with PD173955.
Radicicol The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Radicicol.
Cediranib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Cediranib.
Nilotinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Nilotinib.
Vatalanib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Vatalanib.
Vandetanib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Vandetanib.
Canertinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Canertinib.
Tandutinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Tandutinib.
Motesanib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Motesanib.
Dovitinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Dovitinib.
Glesatinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Glesatinib.
Lestaurtinib The therapeutic efficacy of Palopegteriparatide can be decreased when used in combination with Lestaurtinib.

Target Protein

Parathyroid hormone/parathyroid hormone-related peptide receptor PTH1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 38572533
    Rejnmark L: Treatment of Hypoparathyroidism by Re-Establishing the Effects of Parathyroid Hormone. Endocrinol Metab (Seoul). 2024 Apr;39(2):262-266. doi: 10.3803/EnM.2024.1916. Epub 2024 Apr 4.
  • PMID: 33666947
    Ish-Shalom S, Caraco Y, Khazen NS, Gershinsky M, Szalat A, Schwartz P, Arbit E, Galitzer H, Tang JC, Burshtein G, Rothner A, Raskin A, Blum M, Fraser WD: Safety and Efficacy of Oral Human Parathyroid Hormone (1-34) in Hypoparathyroidism: An Open-Label Study. J Bone Miner Res. 2021 Jun;36(6):1060-1068. doi: 10.1002/jbmr.4274. Epub 2021 Mar 5.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Yorvipath
    Injection, solution • 168 ug/0.56mL • Subcutaneous • US • Approved
  • Yorvipath
    Injection, solution • 294 ug/0.98mL • Subcutaneous • US • Approved
  • Yorvipath
    Injection, solution • 420 ug/1.4mL • Subcutaneous • US • Approved
  • Yorvipath
    Injection, solution • 168 μg/0.56ml • Subcutaneous • EU • Approved
  • Yorvipath
    Injection, solution • 294 μg/0.98ml • Subcutaneous • EU • Approved
  • Yorvipath
    Injection, solution • 420 μg/1.4ml • Subcutaneous • EU • Approved
  • Yorvipath
    Injection, solution • 168 μg/0.56ml • Subcutaneous • EU • Approved
  • Yorvipath
    Injection, solution • 294 μg/0.98ml • Subcutaneous • EU • Approved
Menampilkan 8 dari 9 produk.

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