GS5734
Remdesivir
CAS: 1809249-37-3
Molecular Formula: C27H35N6O8P
GS5734 - Names and Identifiers
GS5734 - Physico-chemical Properties
| Molecular Formula | C27H35N6O8P |
| Molar Mass | 602.58 |
| Density | 1.47±0.1 g/cm3(Predicted) |
| pKa | 12.00±0.70(Predicted) |
| Storage Condition | 2-8℃ |
| Physical and Chemical Properties | Bioactive Remdesivir (GS-5734) is a nucleoside analog with antiviral activity with an EC50 value of 74 nM for SARS-CoV and MERS-CoV in HAE cells and 30 nM for murine hepatitis virus in delayed brain tumor cells. |
| Use | Application status Redcevir is a nucleotide analog prodrug. In vitro experiments and animal model data show that Redsevier inhibits atypical pneumonia (SARS coronavirus), Middle East respiratory syndrome (MERS coronavirus), Ebola coronavirus and many other coronaviruses by inhibiting ribonucleic acid-dependent ribonucleic acid synthase (RNA-derivedRNApolymerase,RdRp). In vitro cell experiments showed that the half effective concentration (IC50) of Ridecivir for novel coronavirus was 0.77 μmol · L-1. However, Redsivir has not been approved for marketing in any country, and its effectiveness and safety have not been confirmed by phase III clinical trials. Only phase II clinical trials are conducted for Ebola virus. |
GS5734 - Reference
| Reference Show more | 1. [IF=5.192] Feng Zhang et al.Human carboxylesterase 1A plays a predominant role in the hydrolytic activation of remdesivir in humans.Chem-Biol Interact. 2022 Jan;351:109744 |
GS5734 - Precautions for patients with renal insufficiency
Each 100 mg vial of Redsevir lyophilized powder contains 3 g of sodium sulfobutyl ether β-cyclodextrin (SBECD), and each 100 mg/20 mL vial of Redsevir solution contains 6 g of SBECD. SBECD is a vector that is eliminated primarily by the kidneys. COVID-19 patients receiving a loading dose of 200 mg raldegravir will receive 6 g to 12 g SBECD depending on the formulation. The amount of SBECD is within the safe threshold for patients with normal renal function. 10 Accumulation of SBECD in patients with impaired renal function may lead to hepatorenal toxicity. Clinicians may consider prioritizing the use of lyophilized powder formulations (which contain less SBECD) in patients with renal impairment.
Because both retegravir formulations contained SBECD, patients with an eGFR<50 mL/min were excluded from some clinical trials of retegravir; others had an eGFR cutoff of less than 30 mL/min. Due to lack of data, the US Food and Drug Administration's product labeling does not recommend the use of raltegravir in patients with eGFR<30 mL/min.
The CATCO study was a multicenter, open-label, randomized controlled trial comparing the use of raltegravir with standard care for adults hospitalized with COVID-19. The study did not exclude patients with renal impairment. A post hoc analysis was performed on 59 patients with baseline eGFR<30 mL/min; 15 of these patients were on dialysis. The median age of the cohort was 74 years. Thirty-four patients received a lyophilized powder formulation of rydrivir for a median duration of 10 days, and 25 patients received standard care. More men were enrolled in the standard-care group, which also had a lower median eGFR at baseline (12.4 mL/min) than patients in the raltegravir group (22.7 mL/min).
Clinical laboratory assessments were performed on Day 5 only. There was no increased risk of nephrotoxicity on day 5 in patients receiving raldegravir compared to patients receiving standard care. There were also no statistically significant differences between the two groups in terms of the need for new dialysis, the need for new mechanical ventilation, or mortality.
The study has limitations, including a small sample size. However, it provides reassurance of safety in patients with renal impairment. This result is consistent with a systematic review of observational studies and other retrospective studies that reported that the use of radecivir was not associated with an increased incidence of adverse effects in patients with COVID-19 with baseline eGFR<30 mL/min. These data suggest that raldegravir can be used in patients with eGFR<30 mL/min if the potential eGFR is <30 mL/min. The benefits outweigh the risks.
Last Update：2023-08-16 23:22:23
GS5734 - Children's Medication Considerations
- Severe acute respiratory syndrome coronavirus type 2 infection is usually milder in children than in adults, and a large proportion of infected children have no symptoms.
- Most non-hospitalized children with COVID-19 do not require any special treatment.
- Observational studies have described the relationship between severe COVID-19 and ≥ 1 comorbid state, including cardiac disease, neurological disease, preterm birth (infants and young children), diabetes, obesity (especially severe obesity), chronic lung disease, feeding tube dependence, and immunocompromised state. Age (<1 year and 10-14 years) and non-white race were also associated with severe illness.
- Most children hospitalized with severe COVID-19 were not fully vaccinated or were not eligible for COVID-19 vaccination.
- Data on the pathogenesis and clinical spectrum of severe acute respiratory syndrome coronavirus 2 infection in children are more limited than in adults.
- Vertical transmission of severe acute respiratory syndrome coronavirus type 2 appears to be rare, but suspected or probable cases of vertical transmission have been described.
- A small proportion of children and young adults infected with severe acute respiratory syndrome coronavirus type 2 may develop multisystemic inflammatory syndrome (MIS-C) in children. Many MIS-C patients require intensive care management. Most children with MIS-C have no underlying comorbidities.
- Data on the prevalence of post-COVID-19 disease in children are limited, but suggest that younger children may have fewer persistent symptoms than older children and adults.
Last Update：2023-08-16 23:22:23
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Spot supply
Product Name: Remdesivir Visit Supplier Webpage Request for quotationCAS: 1809249-37-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Remdesivir Visit Supplier Webpage Request for quotationCAS: 1809249-37-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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