Peringatan Keamanan

The LD50 in rats and mice following intravenous or subcutaneous administration was 42 mg/kg.L44878

One clinical study reported an accidental overdose in a patient who received 400 mcg in one day, which is five times the recommended clinical dose. This patient experienced asthenia, headache, nausea, and vertigo. Serum calcium was not assessed on the day of the overdose, but
on the following day, the patient’s serum calcium was within the normal range. Other symptoms of overdose may include hypercalcemia, nausea, vomiting, dizziness, tachycardia, orthostatic hypotension, and headache. Since there is no specific antidote for abaloparatide overdose, it is recommended that overdose is managed with drug discontinuation, monitoring of serum calcium and phosphorus, and implementation of appropriate supportive measures, such as hydration. Based on the molecular weight, plasma protein binding and volume of distribution, abaloparatide is not expected to be dialyzable.L740

Abaloparatide

DB05084

biotech approved investigational

Deskripsi

Abaloparatide is an N-terminal analog of parathyroid hormone-related protein (PTHrP) A256778 and an agonist at the parathyroid hormone type 1 (PTH1) receptor.L740 It is a synthetic 34 amino acid peptide with 41% homology to human parathyroid hormone 1-34 and human PTHrP 1-34.L740 Abaloparatide and PTHrP share the first 21 amino acids and the receptor-activating domain.A256778

Abaloparatide is an osteoanabolic agent that stimulates bone formation.L740 It was first approved by the FDA on April 28, 2017,A256748 for the treatment of osteoporosis in postmenopausal women and is also used to increase bone density in men with osteoporosis.L740 In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended abaloparatide be granted marketing authorization in Europe L43552 and the drug was fully authorized by the European Commission on December 19, 2022.L44848

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 mean half-life of abaloparatide is approximately one hour.[L740]
Volume Distribusi The volume of distribution was approximately 50 L.[L740]
Klirens (Clearance) The mean apparent total plasma clearance for subcutaneous administration is 168 L/h in healthy subjects.[L44737]

Absorpsi

The absolute bioavailability of abaloparatide in healthy women after subcutaneous administration of an 80 mcg dose was 36%. Following subcutaneous administration of 80 mcg abaloparatide in postmenopausal women with osteoporosis for seven days, the mean (SD) Cmax was 812 (118) pg/mL and the AUC0-24 was 1622 (641) pgxhr/mL. The median Tmax was 0.51 hours, with a range from 0.25 to 0.52 hours.L740

Metabolisme

Abaloparatide is metabolized into smaller peptide fragments via non-specific proteolytic degradation.L740

Rute Eliminasi

The peptide fragments of abaloparatide are primarily eliminated through renal excretion.L740

Interaksi Makanan

3 Data
  • 1. Administer vitamin supplements. If dietary intake is inadequate, patients should receive supplemental calcium and vitamin D.
  • 2. Take at the same time every day.
  • 3. Take with or without food.

Interaksi Obat

307 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Abaloparatide is combined with Duloxetine.
Isoxsuprine The risk or severity of adverse effects can be increased when Abaloparatide is combined with Isoxsuprine.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Abaloparatide.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Abaloparatide.
Celiprolol Abaloparatide may increase the hypotensive activities of Celiprolol.
Epanolol Abaloparatide may increase the hypotensive activities of Epanolol.
Fostamatinib The risk or severity of hypotension can be increased when Fostamatinib is combined with Abaloparatide.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Abaloparatide.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Abaloparatide is combined with Levodopa.
Risperidone Abaloparatide may increase the hypotensive activities of Risperidone.
Aripiprazole Aripiprazole may increase the hypotensive activities of Abaloparatide.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Abaloparatide.
Nicorandil Nicorandil may increase the hypotensive activities of Abaloparatide.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Abaloparatide.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Abaloparatide.
Procaine Procaine may increase the orthostatic hypotensive activities of Abaloparatide.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Abaloparatide.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Abaloparatide.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Abaloparatide.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Abaloparatide.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Abaloparatide.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Abaloparatide.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Abaloparatide.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Abaloparatide.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Abaloparatide.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Abaloparatide.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Abaloparatide.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Abaloparatide.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Abaloparatide.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Abaloparatide.
Methylene blue Methylene blue may increase the orthostatic hypotensive activities of Abaloparatide.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Abaloparatide.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Abaloparatide.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Abaloparatide.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Abaloparatide.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Abaloparatide.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Abaloparatide.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Abaloparatide.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Abaloparatide.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Abaloparatide.
Safrazine Safrazine may increase the orthostatic hypotensive activities of Abaloparatide.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Abaloparatide.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Abaloparatide.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Abaloparatide.
Butabarbital Butabarbital may increase the hypotensive activities of Abaloparatide.
Butalbital Butalbital may increase the hypotensive activities of Abaloparatide.
Pentobarbital Pentobarbital may increase the hypotensive activities of Abaloparatide.
Secobarbital Secobarbital may increase the hypotensive activities of Abaloparatide.
Methohexital Methohexital may increase the hypotensive activities of Abaloparatide.
Thiopental Thiopental may increase the hypotensive activities of Abaloparatide.
Primidone Primidone may increase the hypotensive activities of Abaloparatide.
Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Abaloparatide.
Thiamylal Thiamylal may increase the hypotensive activities of Abaloparatide.
Phenobarbital Phenobarbital may increase the hypotensive activities of Abaloparatide.
Amobarbital Amobarbital may increase the hypotensive activities of Abaloparatide.
Hexobarbital Hexobarbital may increase the hypotensive activities of Abaloparatide.
Barbital Barbital may increase the hypotensive activities of Abaloparatide.
Barbexaclone Barbexaclone may increase the hypotensive activities of Abaloparatide.
Streptokinase The risk or severity of adverse effects can be increased when Streptokinase is combined with Abaloparatide.
Valsartan The risk or severity of adverse effects can be increased when Valsartan is combined with Abaloparatide.
Ramipril The risk or severity of adverse effects can be increased when Ramipril is combined with Abaloparatide.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Abaloparatide.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Abaloparatide.
Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Abaloparatide.
Torasemide The risk or severity of adverse effects can be increased when Torasemide is combined with Abaloparatide.
Methyclothiazide The risk or severity of adverse effects can be increased when Methyclothiazide is combined with Abaloparatide.
Metoprolol The risk or severity of adverse effects can be increased when Metoprolol is combined with Abaloparatide.
Ropinirole The risk or severity of adverse effects can be increased when Ropinirole is combined with Abaloparatide.
Isradipine The risk or severity of adverse effects can be increased when Isradipine is combined with Abaloparatide.
Olmesartan The risk or severity of adverse effects can be increased when Olmesartan is combined with Abaloparatide.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Abaloparatide.
Ropivacaine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Abaloparatide.
Bupivacaine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Abaloparatide.
Chlorthalidone The risk or severity of adverse effects can be increased when Chlorthalidone is combined with Abaloparatide.
Tolcapone The risk or severity of adverse effects can be increased when Tolcapone is combined with Abaloparatide.
Nitroprusside The risk or severity of adverse effects can be increased when Nitroprusside is combined with Abaloparatide.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Abaloparatide.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Abaloparatide.
Diltiazem The risk or severity of adverse effects can be increased when Diltiazem is combined with Abaloparatide.
Minoxidil The risk or severity of adverse effects can be increased when Minoxidil is combined with Abaloparatide.
Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Abaloparatide.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with Abaloparatide.
Amlodipine The risk or severity of adverse effects can be increased when Amlodipine is combined with Abaloparatide.
Triamterene The risk or severity of adverse effects can be increased when Triamterene is combined with Abaloparatide.
Nimodipine The risk or severity of adverse effects can be increased when Nimodipine is combined with Abaloparatide.
Nisoldipine The risk or severity of adverse effects can be increased when Nisoldipine is combined with Abaloparatide.
Pramipexole The risk or severity of adverse effects can be increased when Pramipexole is combined with Abaloparatide.
Spironolactone The risk or severity of adverse effects can be increased when Spironolactone is combined with Abaloparatide.
Nitric Oxide The risk or severity of adverse effects can be increased when Nitric Oxide is combined with Abaloparatide.
Bendroflumethiazide The risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Abaloparatide.
Prazosin The risk or severity of adverse effects can be increased when Prazosin is combined with Abaloparatide.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Abaloparatide.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Abaloparatide.
Nabilone The risk or severity of adverse effects can be increased when Nabilone is combined with Abaloparatide.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Abaloparatide.
Fosinopril The risk or severity of adverse effects can be increased when Fosinopril is combined with Abaloparatide.
Trandolapril The risk or severity of adverse effects can be increased when Trandolapril is combined with Abaloparatide.
Metolazone The risk or severity of adverse effects can be increased when Metolazone is combined with Abaloparatide.
Lercanidipine The risk or severity of adverse effects can be increased when Lercanidipine is combined with Abaloparatide.
Benazepril The risk or severity of adverse effects can be increased when Benazepril is combined with Abaloparatide.

Target Protein

Parathyroid hormone/parathyroid hormone-related peptide receptor PTH1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28624872
    Shirley M: Abaloparatide: First Global Approval. Drugs. 2017 Aug;77(12):1363-1368. doi: 10.1007/s40265-017-0780-7.
  • PMID: 36512663
    Akel M, Parmar M: Abaloparatide. .
  • PMID: 26562265
    Hattersley G, Dean T, Corbin BA, Bahar H, Gardella TJ: Binding Selectivity of Abaloparatide for PTH-Type-1-Receptor Conformations and Effects on Downstream Signaling. Endocrinology. 2016 Jan;157(1):141-9. doi: 10.1210/en.2015-1726. Epub 2015 Nov 12.
  • PMID: 31136739
    Bhattacharyya S, Pal S, Chattopadhyay N: Abaloparatide, the second generation osteoanabolic drug: Molecular mechanisms underlying its advantages over the first-in-class teriparatide. Biochem Pharmacol. 2019 Aug;166:185-191. doi: 10.1016/j.bcp.2019.05.024. Epub 2019 May 25.
  • PMID: 34740971
    Wang MW, Yang Z, Chen X, Zhou SH, Huang GL, Sun JN, Jiang H, Xu WM, Lin HC, Yu X, Sun JP: Activation of PTH1R alleviates epididymitis and orchitis through Gq and beta-arrestin-1 pathways. Proc Natl Acad Sci U S A. 2021 Nov 9;118(45):e2107363118. doi: 10.1073/pnas.2107363118.
  • PMID: 28363951
    Bastepe M, Turan S, He Q: Heterotrimeric G proteins in the control of parathyroid hormone actions. J Mol Endocrinol. 2017 May;58(4):R203-R224. doi: 10.1530/JME-16-0221.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Eladynos
    Injection, solution • 80 mcg/40mcl • Subcutaneous • EU
  • Eladynos
    Injection, solution • 80 μg/dose • Subcutaneous • EU
  • Tymlos
    Injection, solution • 3.12 mg/1.56mL • Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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