Veklury (remdesivir)
COVID-19 (SARS-CoV-2) Antiviral Agents-Nucleotide Analog Intravenous Vial (Ea)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Remdesivir, a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) nucleotide RNA polymerase inhibitor, is an antiviral agent.
Remdesivir, an adenosine nucleotide polymerase inhibitor, is a prodrug that is metabolized intracellularly to form the pharmacologically active nucleoside triphosphate metabolite (GS-443902). The drug is a direct-acting antiviral (DAA).
The mechanism(s) of action of remdesivir against susceptible viruses, including coronaviruses such as SARS-CoV-2 (causative agent of coronavirus disease 2019 (COVID-19)), has not been fully elucidated.
Following conversion of remdesivir to the active triphosphate metabolite (GS-443902), the drug acts as an analog of adenosine triphosphate (ATP) and competes with high selectivity with the natural ATP substrate for incorporation into nascent RNA chains by the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp), which results in delayed chain termination (position I+3) during replication of the viral RNA. Other mechanisms also may be involved. In a biochemical assay assessing incorporation of GS-443902 by the RdRp complex of MERS-CoV (causative agent of Middle East respiratory syndrome (MERS)), RNA synthesis was inhibited with a half-maximal inhibitory concentration (IC50) of 0.032 mcM.
GS-443902 can also inhibit viral RNA synthesis following incorporation into the template viral RNA as a result of read-through by the viral polymerase that may occur at higher nucleotide concentrations. When the remdesivir nucleotide triphosphate is present in the viral RNA template, the efficiency of incorporation of the complementary natural nucleotide is compromised, thereby inhibiting viral RNA synthesis.
Remdesivir triphosphate is a weak inhibitor of mammalian DNA and RNA polymerases, including human mitochondrial RNA polymerase.
USES: Remdesivir is used to treat coronavirus disease, also known as COVID-19, for certain patients who are in the hospital. Remdesivir is an antiviral drug. Remdesivir may also be used to treat patients with COVID-19 who are not in the hospital, but have a high risk for COVID-19 complications due to older age, obesity, or ongoing medical conditions (such as lung, kidney, or heart disease, diabetes).
Generic name: remdesivir
Pronunciation: (rem-DE-si-vir)
Drug class: COVID-19 (SARS-CoV-2) Antiviral Agents-Nucleotide Analog
Therapeutic class: Anti-Infective Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Veklury
Indications
The following indications are listed for Veklury:
- Covid-19
Also known as: Coronavirus Disease, Disease Caused By 2019 Novel Coronavirus, Disease Caused By 2019-Ncov, Disease Caused By Severe Acute Respiratory Syndrome Coronavirus 2, Sars-Cov-2 Infection.
Dosing
No dosing information is available for this tab.
Remdesivir is administered only by IV infusion. The drug should not be given by any other route.
Remdesivir is available in 2 different formulations: a lyophilized powder in single-dose vials containing 100 mg of remdesivir that must be reconstituted with sterile water for injection prior to dilution with 0.9% sodium chloride injection, and a solution concentrate in single-dose vials containing 100 mg/20 mL (5 mg/mL) that must be further diluted in 0.9% sodium chloride injection prior to infusion. Carefully follow the product-specific preparation instructions for each formulation. The lyophilized powder formulation is the only approved dosage form of remdesivir for pediatric patients weighing 3 kg to less than 40 kg.
Remdesivir should not be administered simultaneously with any other IV drugs.
Remdesivir is compatible with 0.9% sodium chloride injection, but compatibility with other IV solutions or drugs is not known.
The manufacturer states that remdesivir solutions should not be shaken. Because studies have not been conducted to assess the effects of vigorous shaking or vibration on the drug, the manufacturer states that pneumatic tube systems should not be used to transport or deliver IV infusion bags containing remdesivir.
After the IV infusion of remdesivir is completed, the infusion line should be flushed with a sufficient volume of 0.9% sodium chloride injection to ensure delivery of the entire dose.
Remdesivir solutions should be inspected visually for discoloration and particulates prior to administration whenever solution and container permit; the solutions should be discarded if they are discolored or contain particulates.
Remdesivir formulations contain no preservatives or bacteriostatic agents. Final dilutions of the drug should be prepared on the same day that they are administered and should be administered immediately after preparation whenever possible. Unused lyophilized powder, solution concentrate, or diluted solutions of the drug should be discarded and should not be reused or saved for future use.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Veklury 100 Mg Vial | Maintenance | Infuse 100 mg by intravenous route once daily. |
No dosing information is available for this tab.
Drug interactions
Drug-drug interaction trials of remdesivir and concomitant medications have not been conducted in humans. The clinical relevance of remdesivir in vitro interaction assessments has not been established.
In vitro, remdesivir is a substrate for cytochrome P-450 (CYP) isoenzyme 3A4, P-glycoprotein (P-gp), and organic anion transporting polypeptide (OATP) 1B1; the predominant circulating metabolite of remdesivir (GS-441524) is a substrate for OATP1B1 and OATP1B3.
In vitro, remdesivir is an inhibitor of CYP3A4, OATP1B1, OATP1B3, and multidrug and toxin extrusion transporter (MATE) 1.
In vitro, remdesivir is not a substrate for CYP1A1, 1A2, 2B6, 2C9, or 2C19. Remdesivir metabolites (GS-704277 and GS-441524) are not substrates for CYP1A1, 1A2, 2B6, 2C8, 2C9, 2D6, or 3A5 and GS-441524 is also not a substrate for CYP2C19 or 3A4. Remdesivir is not a substrate for OATP1B3. GS-704277 and GS-441524 are not substrates for organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 1, OCT2, MATE1, or MATE2K and GS-441524 is also not a substrate for OATP1B1 or OATP1B3.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Remdesivir/Chloroquine; Hydroxychloroquine
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Chloroquine may inhibit the intracellular metabolic activation and antiviral activity of remdesivir.(1,2)
CLINICAL EFFECTS: Concurrent use of chloroquine or hydroxychloroquine may result in decreased effectiveness of remdesivir.(1,2)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The concurrent use of chloroquine or hydroxychloroquine with remdesivir is not recommended.(1,2) Monitor patients receiving concurrent therapy for decreased remdesivir effects.
DISCUSSION: In vitro tests in HEp-2 cells infected with respiratory syncytial virus (RSV) found that the antiviral activity of remdesivir was antagonized by chloroquine phosphate in a dose-dependent manner at clinically relevant concentrations.(1,2) Higher remdesivir EC50 values were seen with increasing concentrations of chloroquine phosphate. Reduced formation of remdesivir triphosphate (the pharmacologically active metabolite) in normal human bronchial epithelial cells was also seen with increasing concentration of chloroquine phosphate.(1,2)
There are no moderate interactions for this drug.
Contraindications
Remdesivir is contraindicated in patients with a history of clinically important hypersensitivity reactions to the drug or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- Sinus bradycardia
Adverse reactions
Adverse effects reported in 5% or more of patients receiving remdesivir include nausea and increased ALT and AST concentrations.
More Frequent
- Increased alanine transaminase
- Increased aspartate transaminase
Less Frequent
- Abnormal hepatic function tests
- Hyperbilirubinemia
Rare or Very Rare
- Anaphylaxis
- Angioedema
- Bradycardia
- Dyspnea
- Extravasation injury
- Hypersensitivity drug reaction
- Hypertension
- Hypotension
- Hypoxia
- Seizure disorder
- Sinus bradycardia
More Frequent
- Nausea
Less Frequent
- Fever
- Hyperglycemia
Rare or Very Rare
- Chills
- Hyperhidrosis
- Skin rash
- Tachycardia
- Vomiting
- Wheezing
Precautions
No enhanced messaging available.
Safety and efficacy of remdesivir for the treatment of COVID-19 have been established in pediatric patients 28 days of age and older weighing at least 3 kg. Use of the drug in this pediatric population is supported by an open-label trial in 53 hospitalized pediatric subjects who were treated for up to 10 days with weight-based remdesevir. Safety and pharmacokinetic findings in this age group were similar to those in adults. Use of remdesivir in pediatric patients weighing at least 40 kg is futher supported by a clinical trial in nonhospitalized patients that included 3 pediatric patients 12 years of age and older and by clinical trials in hospitalized patients that included 30 adults weighing 40 to 50 kg.
Use of remdesivir in pediatric patients with renal impairment is supported by safety data in adults. There are limited data in pediatric patients with mild to moderate renal impairment and no data in pediatric patients with severe renal impairment. The formulation contains the excipient betadex sulfobutyl ether sodium (sulfobutylether beta-cyclodextrin sodium; SBECD) which, when administeredIV, is eliminated through glomerular filtration and therefore when administered to pediatricpatients with renal immaturity or renal impairment, may result in higher exposure to SBECD.
Data regarding the use of remdesivir during pregnancy are available from a clinical trial, published case reports, an ongoing pregnancy exposure registry, and a compassionate use access program. The available data have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes following drug exposure in the second and third trimester; however, there are insufficient data regarding risk during the first trimester. There are maternal and fetal risks associated with untreated COVID-19 during pregnancy.
In nonclinical reproductive toxicity studies, remdesivir demonstrated no adverse effect on embryofetal development when administered to pregnant animals at systemic exposures of the predominant circulating metabolite of remdesivir (GS-441524) that were 4 times (rats and rabbits) the exposure in humans at the recommended human dose (RHD).
Some data are available regarding use of remdesivir in pregnant women hospitalized for the treatment of moderate COVID-19.
Remdesivir and its active metabolite distribute into human milk; however, available data do not indicate any adverse effects on the breast-fed infant from exposure to the drug. It is not known whether remdesivir has any effects on milk production.
The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for remdesivir and any potential adverse effects on the breast-fed child from the drug or from the underlying maternal condition. Breastfeeding individuals with COVID-19 should follow clinical guidelines to avoid exposing the infant to the virus.
Dosage adjustment of remdesivir is not needed in patients older than 65 years of age; however, the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly should be considered.
Reported clinical experience has not identified differences in responses to remdesivir between geriatric and younger patients. Although dosage adjustment of remdesivir is not needed in patients older than 65 years of age, appropriate caution and monitoring are recommended because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease or other drug therapy observed in this age group.
ICD codes
| Code | Type | Description |
|---|---|---|
| COVId-19 | ||
| J12.82 | ICD10CM | Pneumonia due to coronavirus disease 2019 |
| U07.1 | ICD10CM | COVId-19 |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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