remdesivir Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals 5376 1809249-37-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • veklury
  • captisol-enabled remdesivir
  • captisol-enabled GS 5734
  • remdesivir
  • GS-5734
Remdesivir is an investigational nucleotide analog with broad-spectrum antiviral activity. Remdesivir has demonstrated in vitro and in vivo activity in animal models against the viral pathogens MERS and SARS, which are also coronaviruses and are structurally similar to COVID-19. The limited preclinical data on remdesivir in MERS and SARS indicate that remdesivir may have potential activity against COVID-19. The only direct-acting antiviral (DAA) currently approved by FDA for the treatment of COVID-19 in certain populations.
  • Molecular weight: 602.59
  • Formula: C27H35N6O8P
  • CLOGP: 1.25
  • LIPINSKI: 2
  • HAC: 14
  • HDO: 4
  • TPSA: 203.55
  • ALOGS: -3.25
  • ROTB: 14

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 7, 2020 EMA Gilead Sciences Ireland UC
Oct. 22, 2020 FDA GILEAD SCIENCES INC
May 7, 2020 PMDA Gilead Sciences K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Alanine aminotransferase increased 791.72 43.73 301 4174 88150 46593437
Aspartate aminotransferase increased 521.07 43.73 216 4259 78484 46603103
Liver function test increased 454.94 43.73 142 4333 22684 46658903
Infusion site extravasation 199.25 43.73 54 4421 5202 46676385
Blood creatinine increased 196.55 43.73 110 4365 76293 46605294
COVID-19 193.01 43.73 71 4404 18504 46663083
Bradycardia 188.51 43.73 102 4373 66196 46615391
Acute kidney injury 177.85 43.73 160 4315 235695 46445892
COVID-19 pneumonia 174.01 43.73 44 4431 3231 46678356
Therapy cessation 171.55 43.73 72 4403 26557 46655030
Glomerular filtration rate decreased 137.49 43.73 49 4426 11645 46669942
Transaminases increased 129.97 43.73 60 4415 27701 46653886
Death 110.04 43.73 147 4328 335401 46346186
Therapy interrupted 100.13 43.73 38 4437 10753 46670834
Renal impairment 88.40 43.73 66 4409 74306 46607281
Product preparation error 88.08 43.73 27 4448 4012 46677575
Hypoxia 80.07 43.73 54 4421 51784 46629803
Respiratory failure 76.31 43.73 67 4408 94749 46586838
Cardiac arrest 67.02 43.73 61 4414 90338 46591249
Extravasation 62.99 43.73 18 4457 2097 46679490
Acute respiratory distress syndrome 60.09 43.73 33 4442 21889 46659698
Clinical trial participant 59.54 43.73 8 4467 10 46681577
Premature delivery 54.44 43.73 31 4444 22038 46659549
Oxygen saturation decreased 53.85 43.73 48 4427 69116 46612471
Acute respiratory failure 51.39 43.73 33 4442 29105 46652482
Product preparation issue 51.11 43.73 11 4464 396 46681191
Pulseless electrical activity 44.80 43.73 19 4456 7148 46674439

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Alanine aminotransferase increased 1648.92 48.23 626 6531 73650 29871671
Aspartate aminotransferase increased 898.53 48.23 389 6768 63033 29882288
Liver function test increased 868.11 48.23 245 6912 10971 29934350
Bradycardia 304.59 48.23 191 6966 65335 29879986
Therapy cessation 301.28 48.23 119 7038 15018 29930303
Blood creatinine increased 271.54 48.23 202 6955 91173 29854148
Acute kidney injury 235.58 48.23 306 6851 273536 29671785
COVID-19 210.77 48.23 97 7060 17781 29927540
Therapy interrupted 202.57 48.23 65 7092 4464 29940857
Transaminases increased 185.75 48.23 97 7060 23360 29921961
Hepatic enzyme increased 181.75 48.23 108 7049 33386 29911935
COVID-19 pneumonia 166.16 48.23 56 7101 4484 29940837
Respiratory failure 151.61 48.23 151 7006 100491 29844830
Glomerular filtration rate decreased 150.80 48.23 67 7090 11295 29934026
Hypoxia 126.66 48.23 99 7058 47755 29897566
Infusion site extravasation 124.47 48.23 39 7118 2474 29942847
Death 122.84 48.23 265 6892 357018 29588303
Product preparation error 116.89 48.23 34 7123 1672 29943649
Clinical trial participant 101.29 48.23 18 7139 82 29945239
Cardiac arrest 87.23 48.23 109 7048 92741 29852580
Pulseless electrical activity 80.50 48.23 36 7121 6151 29939170
Product preparation issue 79.58 48.23 16 7141 155 29945166
Acute respiratory distress syndrome 76.35 48.23 55 7102 23417 29921904
COVID-19 treatment 70.62 48.23 16 7141 284 29945037
Oxygen saturation decreased 70.43 48.23 68 7089 43372 29901949
Acute respiratory failure 69.42 48.23 54 7103 25796 29919525
Hypertransaminasaemia 64.97 48.23 27 7130 3858 29941463
Haemodialysis 60.70 48.23 36 7121 11037 29934284
Palliative care 57.66 48.23 14 7143 339 29944982
Blood bilirubin increased 54.98 48.23 55 7102 36581 29908740
Fatigue 53.21 48.23 7 7150 320666 29624655
Renal impairment 52.21 48.23 81 7076 84103 29861218

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000963 Antimetabolites
MeSH PA D000998 Antiviral Agents
MeSH PA D009676 Noxae
CHEBI has role CHEBI:36044 anti-virus drug
CHEBI has role CHEBI:50266 prodrugs
CHEBI has role CHEBI:149553 anti-coronaviral agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Disease caused by Severe acute respiratory syndrome coronavirus 2 indication 840539006
Coronavirus infection off-label use 186747009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.68 acidic
pKa2 12.82 acidic
pKa3 4.2 Basic
pKa4 1.68 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG/20ML (5MG/ML) VEKLURY GILEAD SCIENCES INC N214787 Oct. 22, 2020 RX SOLUTION INTRAVENOUS Oct. 22, 2025 NEW CHEMICAL ENTITY
100MG/VIAL VEKLURY GILEAD SCIENCES INC N214787 Oct. 22, 2020 RX POWDER INTRAVENOUS Oct. 22, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Ebola virus (EBOV) Virus INHIBITOR EC50 7.06 SCIENTIFIC LITERATURE

External reference:

IDSource
4039395 VANDF
4039396 VANDF
C4279131 UMLSCUI
CHEBI:145994 CHEBI
CHEMBL4065616 ChEMBL_ID
DB14761 DRUGBANK_ID
C000606551 MESH_SUPPLEMENTAL_RECORD_UI
D11472 KEGG_DRUG
10715 IUPHAR_LIGAND_ID
10478 INN_ID
3QKI37EEHE UNII
121304016 PUBCHEM_CID
2284718 RXNORM
333266 MMSL
336406 MMSL
38322 MMSL
d09540 MMSL
018308 NDDF
870518005 SNOMEDCT_US
870592005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Veklury HUMAN PRESCRIPTION DRUG LABEL 1 61958-2901 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS unapproved drug other 28 sections
Veklury HUMAN PRESCRIPTION DRUG LABEL 1 61958-2901 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS unapproved drug other 28 sections
Veklury HUMAN PRESCRIPTION DRUG LABEL 1 61958-2902 INJECTION 5 mg INTRAVENOUS unapproved drug other 28 sections
Veklury HUMAN PRESCRIPTION DRUG LABEL 1 61958-2902 INJECTION 5 mg INTRAVENOUS unapproved drug other 28 sections