tecovirimat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals 5291 869572-92-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tecovirimat
  • tpoxx
  • siga-246
  • ST-246
  • tecovirimat monohydrate
Tecovirimat targets and inhibits the activity of the orthopoxvirus VP37 protein (encoded by and highly conserved in all members of the orthopoxvirus genus) and blocks its interaction with cellular Rab9 GTPase and TIP47, which prevents the formation of egress-competent enveloped virions necessary for cell-to-cell and long-range dissemination of virus.
  • Molecular weight: 376.34
  • Formula: C19H15F3N2O3
  • CLOGP: 2.94
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 66.48
  • ALOGS: -4.25
  • ROTB: 3

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Jan. 6, 2022 EMA SIGA TECHNOLOGIES NETHERLANDS B.V.
July 13, 2018 FDA SIGA TECHNOLOGIES

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AX24 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Other antivirals
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190118 Cytochrome P450 3A Inducers
FDA EPC N0000193857 Orthopoxvirus VP37 Envelope Wrapping Protein Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Smallpox indication 67924001 DOID:8736
Cowpox indication 70090004 DOID:8956
Monkeypox indication 359814004 DOID:3292
Complications due to replication of vaccinia virus following vaccination against smallpox indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.13 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
200MG TPOXX SIGA TECHNOLOGIES N208627 July 13, 2018 RX CAPSULE ORAL 8802714 June 18, 2024 TREATMENT OF HUMAN SMALLPOX DISEASE CAUSED BY VARIOLA VIRUS IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 13 KG
200MG/20ML (10MG/ML) TPOXX SIGA TECHNOLOGIES N214518 May 18, 2022 RX SOLUTION INTRAVENOUS 8802714 June 18, 2024 TPOXX IS INDICATED FOR THE TREATMENT OF HUMAN SMALLPOX DISEASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 3 KG
200MG/20ML (10MG/ML) TPOXX SIGA TECHNOLOGIES N214518 May 18, 2022 RX SOLUTION INTRAVENOUS 9907859 Aug. 2, 2031 TPOXX IS INDICATED FOR THE TREATMENT OF HUMAN SMALLPOX DISEASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 3 KG
200MG TPOXX SIGA TECHNOLOGIES N208627 July 13, 2018 RX CAPSULE ORAL 7737168 Sept. 4, 2031 TREATMENT OF HUMAN SMALLPOX DISEASE CAUSED BY VARIOLA VIRUS IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 13 KG
200MG/20ML (10MG/ML) TPOXX SIGA TECHNOLOGIES N214518 May 18, 2022 RX SOLUTION INTRAVENOUS 7737168 Sept. 4, 2031 TPOXX IS INDICATED FOR THE TREATMENT OF HUMAN SMALLPOX DISEASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 3 KG

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
200MG TPOXX SIGA TECHNOLOGIES N208627 July 13, 2018 RX CAPSULE ORAL July 13, 2023 NEW CHEMICAL ENTITY
200MG/20ML (10MG/ML) TPOXX SIGA TECHNOLOGIES N214518 May 18, 2022 RX SOLUTION INTRAVENOUS July 13, 2023 NEW CHEMICAL ENTITY
200MG TPOXX SIGA TECHNOLOGIES N208627 July 13, 2018 RX CAPSULE ORAL July 13, 2025 INDICATED FOR THE TREATMENT OF HUMAN SMALLPOX DISEASE CAUSED BY VARIOLA VIRUS IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 13 KG

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Envelope protein F13 Viral envelope protein INHIBITOR EC50 7.38 DRUG LABEL DRUG LABEL

External reference:

IDSource
F925RR824R UNII
1162664-19-8 SECONDARY_CAS_RN
C2713595 UMLSCUI
CHEMBL1257073 ChEMBL_ID
CHEMBL1242629 ChEMBL_ID
16124688 PUBCHEM_CID
DB12020 DRUGBANK_ID
D09390 KEGG_DRUG
9011 INN_ID
40695 MMSL
d09893 MMSL
017694 NDDF
772991002 SNOMEDCT_US
773289005 SNOMEDCT_US
4039493 VANDF
2055104 RXNORM
C505045 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-010 INJECTION, SOLUTION, CONCENTRATE 10 mg INTRAVENOUS NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-010 INJECTION, SOLUTION, CONCENTRATE 10 mg INTRAVENOUS NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-010 INJECTION, SOLUTION, CONCENTRATE 10 mg INTRAVENOUS NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-200 CAPSULE 200 mg ORAL NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-200 CAPSULE 200 mg ORAL NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-200 CAPSULE 200 mg ORAL NDA 30 sections
TPOXX HUMAN PRESCRIPTION DRUG LABEL 1 50072-200 CAPSULE 200 mg ORAL NDA 30 sections