Peringatan Keamanan

In mice, subcutaneous administration of nedosiran at doses up to 2000 mg/kg/dose (approximately 58 times the maximum recommended human dose (MRHD) based on body surface area (BSA)) or a mouse-specific (pharmacologically active) analog (10 mg/kg/dose) during organogenesis (dosing on gestation days 6, 8, 10, 12, and 14 for nedosiran; gestation days 3 and 10 for the analog) did not have adverse effects on embryofetal development.L48320

Subcutaneous administration of nedosiran (0, 2, 6, or 20 mg/kg/dose) to pregnant rabbits during organogenesis (dosing on gestation days 7, 9, 11, 13, 15, 17, and 19) resulted in maternal toxicity on the basis of body weight loss of up to 6.5% following the first dose in the 6 and 20 mg/kg/dose groups. Higher post-implantation loss and lower numbers of live fetuses occurred at ? 6 mg/kg/dose (exposures equivalent to the MRHD based on BSA), and fetal cardiovascular and skeletal malformations occurred at the 20 mg/kg/dose (2 times the MRHD based on BSA). No adverse findings were seen at the 2 mg/kg/dose, which is below the MRHD.L48320

In a pre-and postnatal study in mice, subcutaneous administration of nedosiran (0, 250, 500, or 1000 mg/kg/dose) or a mouse-specific (pharmacologically active) analog (10 mg/kg/dose) from implantation (dosing on gestational days 6, 8, 10, 12, 14, 16) to weaning (dosing on lactation days 1, 8 15, 20) did not have adverse effects on the growth, viability, development and reproductive performance of the offspring.L48320

Long-term studies to assess the carcinogenic risk of nedosiran have not been conducted.L48320

Nedosiran was not genotoxic in the in vitro bacterial mutagenicity, in vitro micronucleus assays (human peripheral blood lymphocytes), and in vivo bone marrow micronucleus assay in mice.L48320

Weekly subcutaneous administration of nedosiran at doses of 500, 1000, or 2000 mg/kg or of a mouse-specific (pharmacologically active) analog at a dose of 10 mg/kg to male mice for 4 weeks prior to and throughout mating, and to female mice for 2 weeks prior to and throughout mating and to gestation day 7 did not affect male or female fertility or early embryonic development.L48320

Nedosiran

DB17635

biotech approved investigational

Deskripsi

Nedosiran is an RNA interference targeting hepatic lactate dehydrogenase, the enzyme responsible for the conversion of glyoxylate to oxalate.A261690 Oxalate, particularly calcium oxalate, precipitation is the main cause of kidney stones formation; therefore, blocking the production of oxalate can help alleviate renal symptoms.A261685

Nedosiran was approved by the FDA on October 2nd, 2023, under the brand name RIVFLOZA to lower urinary oxalate levels in children 9 years of age and older and adults with primary hyperoxaluria type 1 (PH1) and relatively preserved kidney function. This approval is based on the favorable results from the pivotal phase 2 PHYOXTM2 and interim data from the ongoing phase 3 PHYOXTM3 clinical trials.L48325

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of nedosiran was estimated to be 15 hours.[L48320]
Volume Distribusi The volume of distribution was calculated to be 126 L.[L48320]
Klirens (Clearance) The clearance of nedosiran was calculated to be 5.7 L/hr.[L48320]

Absorpsi

Nedosiran exhibited a dose-proportional increase in plasma exposure following single subcutaneous doses from 1.5 to 6.0 mg/kg.L48320 Nedosiran exhibited time-independent pharmacokinetics with multiple doses of 160 mg once monthly (body weight ? 50 kg), 128 mg once monthly (body weight < 50 kg), or 3.3 mg/kg once monthly in the age range of 6 to 11 years.L48320 Other pharmacokinetic parameters like Cmax, AUC0-last, and Tmax were calculated to be 844 ng/mL, 13600 ng*h/mL, and 6 hours respectively.L48320

Metabolisme

As an antisense oligonucleotide, nedosiran is expected to be metabolized by endo- and exonucleases to shorter oligonucleotides.L48320

Rute Eliminasi

Approximately 27% of the administered nedosiran dose is excreted unchanged into the urine within 24 hours of dosing.L48320

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

L-lactate dehydrogenase A chain LDHA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27188687
    Khan SR, Pearle MS, Robertson WG, Gambaro G, Canales BK, Doizi S, Traxer O, Tiselius HG: Kidney stones. Nat Rev Dis Primers. 2016 Feb 25;2:16008. doi: 10.1038/nrdp.2016.8.
  • PMID: 36407951
    Liu A, Zhao J, Shah M, Migliorati JM, Tawfik SM, Bahal R, Rasmussen TP, Manautou JE, Zhong XB: Nedosiran, a Candidate siRNA Drug for the Treatment of Primary Hyperoxaluria: Design, Development, and Clinical Studies. ACS Pharmacol Transl Sci. 2022 Sep 21;5(11):1007-1016. doi: 10.1021/acsptsci.2c00110. eCollection 2022 Nov 11.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Rivfloza
    Injection, solution • 160 mg/1mL • Subcutaneous • US • Approved
  • Rivfloza
    Injection, solution • 128 mg/0.8mL • Subcutaneous • US • Approved
  • Rivfloza
    Injection, solution • 80 mg/0.5mL • Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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