fostemsavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 5401 | 864953-29-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolyzed to the active moiety, temsavir, which is an HIV-1 attachment inhibitor. Temsavir binds directly to the gp120 subunit within the HIV-1 envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular CD4 receptors, thereby preventing attachment. Additionally, temsavir can inhibit gp120-dependent post-attachment steps required for viral entry into host cells.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 250 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 4, 2021 | EMA | ViiV HEALTHCARE B.V. | |
| July 2, 2020 | FDA | ViiV Healthcare Company |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Virologic failure | 130.06 | 94.77 | 20 | 101 | 3460 | 34953350 |
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AX29 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D023581 | HIV Fusion Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus I infection | indication | 40780007 | |
| Drug induction of cytochrome p450 CYP3A enzyme | contraindication | 423236002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 600MG BASE | RUKOBIA | VIIV HLTHCARE | N212950 | July 2, 2020 | RX | TABLET, EXTENDED RELEASE | ORAL | July 2, 2025 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.66 | CHEMBL | |||||
| Envelope glycoprotein gp160 | Viral envelope protein | INHIBITOR | Kd | 9.08 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 | Unclassified | Kd | 9.08 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10707 | KEGG_DRUG |
| 97IQ273H4L | UNII |
| 864953-39-9 | SECONDARY_CAS_RN |
| C4519220 | UMLSCUI |
| CHEMBL3301594 | ChEMBL_ID |
| 11319217 | PUBCHEM_CID |
| DB11796 | DRUGBANK_ID |
| CHEMBL3301598 | ChEMBL_ID |
| CHEMBL3301620 | ChEMBL_ID |
| C584152 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11100 | IUPHAR_LIGAND_ID |
| 018436 | NDDF |
| 018437 | NDDF |
| 1105971000202108 | SNOMEDCT_US |
| 890266008 | SNOMEDCT_US |
| 890270000 | SNOMEDCT_US |
| 4039527 | VANDF |
| C3712177 | UMLSCUI |
| 2380373 | RXNORM |
| 336206 | MMSL |
| 38617 | MMSL |
| d09591 | MMSL |
| C576364 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11317439 | PUBCHEM_CID |
| 10292 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rukobia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-250 | TABLET, FILM COATED, EXTENDED RELEASE | 600 mg | ORAL | NDA | 27 sections |
| Rukobia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-250 | TABLET, FILM COATED, EXTENDED RELEASE | 600 mg | ORAL | NDA | 27 sections |
| Rukobia | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-250 | TABLET, FILM COATED, EXTENDED RELEASE | 600 mg | ORAL | NDA | 27 sections |