doravirine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 5295 | 1338225-97-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Doravirine is a pyridinone non-nucleoside reverse transcriptase inhibitor of HIV-1 and inhibits HIV-1 replication by non-competitive inhibition of HIV-1 reverse transcriptase (RT). Doravirine does not inhibit the human cellular DNA polymerases alpha, beta, and mitochondrial DNA polymerase gamma.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 22, 2018 | EMA | MERCK SHARP & DOHME B.V. | |
| Aug. 30, 2018 | FDA | MSD MERCK CO | |
| Jan. 14, 2020 | PMDA | MSD K.K. |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Pathogen resistance | 58.06 | 57.84 | 10 | 105 | 6388 | 63482519 |
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 |
|---|---|---|---|---|---|---|
| Blood HIV RNA increased | 67.52 | 57.89 | 11 | 243 | 1219 | 34955458 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Blood HIV RNA increased | 87.32 | 68.35 | 13 | 249 | 1795 | 79742331 |
| Pathogen resistance | 71.93 | 68.35 | 15 | 247 | 14327 | 79729799 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AG06 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Non-nucleoside reverse transcriptase inhibitors |
| ATC | J05AR24 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| FDA MoA | N0000009948 | Non-Nucleoside Reverse Transcriptase Inhibitors |
| FDA EXT | N0000175460 | Non-Nucleoside Analog |
| FDA EPC | N0000175463 | Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.92 | acidic |
| pKa2 | 5.15 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG | PIFELTRO | MSD MERCK CO | N210806 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 AS A REPLACEMENT THERAPY IN VIROLOGICALLY SUPPRESSED ADULTS WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO DORAVIRINE |
| 100MG | PIFELTRO | MSD MERCK CO | N210806 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY |
| 100MG | PIFELTRO | MSD MERCK CO | N210806 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | FOR USE IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS TO TREAT HIV-1 INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 35KG WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IF VIROLOGICALLY SUPPRESSED |
| 100MG;300MG;300MG | DELSTRIGO | MSD MERCK CO | N210807 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | FOR THE TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY |
| 100MG;300MG;300MG | DELSTRIGO | MSD MERCK CO | N210807 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | TREATMENT OF HIV-1 INFECTION IN ADULT PATIENTS AS A REPLACEMENT THERAPY IN VIROLOGICALLY SUPPRESSED ADULTS WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INDIVIDUAL COMPONENTS OF DELSTRIGO |
| 100MG;300MG;300MG | DELSTRIGO | MSD MERCK CO | N210807 | Aug. 30, 2018 | RX | TABLET | ORAL | 8486975 | Oct. 7, 2031 | TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 35KG WITH NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG | PIFELTRO | MSD MERCK CO | N210806 | Aug. 30, 2018 | RX | TABLET | ORAL | Aug. 30, 2023 | NEW CHEMICAL ENTITY |
| 100MG;300MG;300MG | DELSTRIGO | MSD MERCK CO | N210807 | Aug. 30, 2018 | RX | TABLET | ORAL | Aug. 30, 2023 | NEW CHEMICAL ENTITY |
| 100MG | PIFELTRO | MSD MERCK CO | N210806 | Aug. 30, 2018 | RX | TABLET | ORAL | Jan. 27, 2025 | NEW PATIENT POPULATION |
| 100MG;300MG;300MG | DELSTRIGO | MSD MERCK CO | N210807 | Aug. 30, 2018 | RX | TABLET | ORAL | Jan. 27, 2025 | NEW PATIENT POPULATION |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Reverse transcriptase/RNaseH | Enzyme | INHIBITOR | EC50 | 7.92 | DRUG LABEL | DRUG LABEL | |||
| Reverse transcriptase | Enzyme | IC50 | 7.72 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 913P6LK81M | UNII |
| C4045491 | UMLSCUI |
| 2KW | PDB_CHEM_ID |
| CHEMBL2364608 | ChEMBL_ID |
| 58460047 | PUBCHEM_CID |
| DB12301 | DRUGBANK_ID |
| D10624 | KEGG_DRUG |
| 9797 | INN_ID |
| 12679 | IUPHAR_LIGAND_ID |
| 288957 | MMSL |
| 34854 | MMSL |
| d08872 | MMSL |
| 017702 | NDDF |
| 781493004 | SNOMEDCT_US |
| 781500009 | SNOMEDCT_US |
| 4037847 | VANDF |
| 2055755 | RXNORM |
| C000592662 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PIFELTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3069 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 30 sections |
| PIFELTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3069 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 30 sections |
| DELSTRIGO | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0006-5007 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
| DELSTRIGO | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0006-5007 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
| PIFELTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-6237 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 29 sections |
| PIFELTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-6268 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 29 sections |