All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

doravirine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
antivirals	5295	1338225-97-0

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: doravirine pifeltro MK-1439

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. Molecular weight: 425.75 Formula: C17H11ClF3N5O3 CLOGP: 2.07 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 98.03 ALOGS: -5.12 ROTB: 5 Status: ONP 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AXL,CDK5,CDK9,EIF2AK3,GRK2,MAPK7,PDK1,PDK2,PDK4,PRKDC	11
kinase-selectivity-class	GRK2	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	1

Approvals:

Date	Agency	Company	Orphan
Jan. 14, 2020	PMDA	MSD K.K.
Aug. 30, 2018	FDA	MSD MERCK CO
Nov. 22, 2018	EMA	MERCK SHARP & DOHME B.V.

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
Virologic failure	75.18	50.35	11	172	2213	90626051
Pathogen resistance	60.95	50.35	11	172	8104	90620160
Treatment noncompliance	55.22	50.35	14	169	51713	90576551
Viral mutation identified	52.81	50.35	8	175	2017	90626247

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	99.05	47.14	17	486	1574	42619258
CD4 lymphocytes decreased	57.17	47.14	11	492	1910	42618922
Drug resistance	51.05	47.14	18	485	34230	42586602

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	123.46	49.59	19	523	2169	110586588
Viral mutation identified	89.94	49.59	16	526	4403	110584354
Pathogen resistance	73.11	49.59	17	525	17655	110571102
CD4 lymphocytes decreased	68.71	49.59	12	530	2962	110585795
Drug resistance	66.28	49.59	20	522	56354	110532403
Treatment noncompliance	57.16	49.59	19	523	72971	110515786
Virologic failure	56.42	49.59	11	531	4941	110583816
Viral load abnormal	50.05	49.59	6	536	102	110588655

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
CHEBI has role	CHEBI:22587	antiviral agent
CHEBI has role	CHEBI:64946	anti-HIV agent
CHEBI has role	CHEBI:231911	renoprotective agent

Related Drugs by ATC class:

J05AG Non-nucleoside reverse transcriptase inhibitors 5 drugs

delavirdineefavirenzetravirinenevirapinerilpivirine

J05AR Antivirals for treatment of HIV infections, combinations 19 drugs

abacaviratazanavirbictegravircobicistatdarunavirdolutegravirefavirenzelvitegraviremtricitabinelamivudinelopinavirnevirapine show all 19 →

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	Aug. 30, 2032	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	Aug. 30, 2032	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	Aug. 30, 2032	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	Aug. 30, 2032	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	Aug. 30, 2032	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	Aug. 30, 2032	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
100MG;0.25MG	IDVYNSO	MSD	N216964	April 20, 2026	RX	TABLET	ORAL	8486975	Aug. 30, 2032	USE OF A COMPLETE TWO-DRUG REGIMEN FOR THE TREATMENT OF HIV-1 INFECTION IN ADULTS TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY-SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG;0.25MG	IDVYNSO	MSD	N216964	April 20, 2026	RX	TABLET	ORAL	April 20, 2031	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Reverse transcriptase/RNaseH	Enzyme		Q72547_9HIV1	INHIBITOR	EC50	7.92		DRUG LABEL	DRUG LABEL
Reverse transcriptase	Enzyme		Q9WKE8_9HIV1		IC50	7.72		CHEMBL

External reference:

ID	Source
913P6LK81M	UNII
4037847	VANDF
C4045491	UMLSCUI
CHEBI:754975	CHEBI
2KW	PDB_CHEM_ID
CHEMBL2364608	ChEMBL_ID
58460047	PUBCHEM_CID
DB12301	DRUGBANK_ID
D10624	KEGG_DRUG
9797	INN_ID
C000592662	MESH_SUPPLEMENTAL_RECORD_UI
12679	IUPHAR_LIGAND_ID
781493004	SNOMEDCT_US
781500009	SNOMEDCT_US
288957	MMSL
34854	MMSL
d08872	MMSL
017702	NDDF
2055755	RXNORM

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	31 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
IDVYNSO	HUMAN PRESCRIPTION DRUG LABEL	2	0006-5092	TABLET, FILM COATED	100 mg	ORAL	NDA	31 sections
PIFELTRO	HUMAN PRESCRIPTION DRUG LABEL	1	50090-6268	TABLET, FILM COATED	100 mg	ORAL	NDA	30 sections