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

Stem definition	Drug id	CAS RN
antivirals phosphonic acid derivatives	4944	379270-37-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GS 7340 tenofovir alagenamide tenofovir alafenamide tenofovir alafenamide fumarate GS-7340	a phosphonoamidate prodrug of tenofovir (2'deoxyadenosine monophosphate analog). Plasma exposure to tenofovir alafenamide allows for permeation into cells and then tenofovir alafenamide is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination Molecular weight: 476.47 Formula: C21H29N6O5P CLOGP: 2.18 LIPINSKI: 1 HAC: 11 HDO: 2 TPSA: 143.48 ALOGS: -3.30 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GS 7340
tenofovir alagenamide
tenofovir alafenamide
tenofovir alafenamide fumarate
GS-7340

a phosphonoamidate prodrug of tenofovir (2'deoxyadenosine monophosphate analog). Plasma exposure to tenofovir alafenamide allows for permeation into cells and then tenofovir alafenamide is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination

Molecular weight: 476.47
Formula: C21H29N6O5P
CLOGP: 2.18
LIPINSKI: 1
HAC: 11
HDO: 2
TPSA: 143.48
ALOGS: -3.30
ROTB: 12

Status: OFP

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

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

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Property	Value	Reference
S (Water solubility)	4.70 mg/mL	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	2 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Dec. 19, 2016	PMDA	Gilead Sciences
Feb. 20, 2014	EMA
Nov. 5, 2015	FDA	GILEAD SCIENCES INC

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FDA Adverse Event Reporting System (Female)

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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
Maternal exposure during pregnancy	56.41	32.11	37	913	220025	63268047
Hepatitis B DNA increased	37.78	32.11	6	944	267	63487805
Viral load increased	33.86	32.11	7	943	1367	63486705

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FDA Adverse Event Reporting System (Male)

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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
Immune reconstitution inflammatory syndrome	86.92	29.67	27	1595	8732	34946577
Hepatitis B DNA increased	67.76	29.67	13	1609	552	34954757
Viral load increased	57.96	29.67	15	1607	2512	34952797
Hepatocellular carcinoma	53.45	29.67	18	1604	7491	34947818
Fanconi syndrome acquired	51.45	29.67	13	1609	1978	34953331
Product storage error	37.04	29.67	14	1608	8108	34947201
Lung transplant rejection	35.12	29.67	8	1614	784	34954525
Pulmonary venous thrombosis	34.95	29.67	6	1616	135	34955174
Hepatitis B	33.52	29.67	12	1610	5971	34949338
HIV associated nephropathy	29.80	29.67	6	1616	327	34954982

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FDA Adverse Event Reporting System (Geriatric)

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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
Hepatitis B DNA increased	102.15	26.19	18	2217	797	79741356
Hepatocellular carcinoma	59.10	26.19	18	2217	9003	79733150
Fanconi syndrome acquired	48.93	26.19	12	2223	2682	79739471
Viral mutation identified	44.65	26.19	12	2223	3846	79738307
Hepatitis B	43.59	26.19	14	2221	8318	79733835
Drug resistance	40.68	26.19	21	2214	42192	79699961
Off label use	37.81	26.19	80	2155	907135	78835018
Pulmonary venous thrombosis	37.28	26.19	6	2229	152	79742001
Product dispensing error	37.22	26.19	14	2221	13249	79728904
Lung transplant rejection	33.88	26.19	8	2227	1523	79740630

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	J05AF13	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Nucleoside and nucleotide reverse transcriptase inhibitors
ATC	J05AR17	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR18	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR19	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR20	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR22	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:53756	reverse transcriptase inhibitors
CHEBI has role	CHEBI:50266	Prodrugs
MeSH PA	D019380	Anti-HIV Agents

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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	4.86	Basic
pKa2	3.96	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
120MG;EQ 15MG BASE	DESCOVY	GILEAD SCIENCES INC	N208215	Jan. 7, 2022	RX	TABLET	ORAL	8754065	Aug. 15, 2032	TREATMENT OF HIV-1 INFECTION
120MG;EQ 15MG BASE	DESCOVY	GILEAD SCIENCES INC	N208215	Jan. 7, 2022	RX	TABLET	ORAL	9296769	Aug. 15, 2032	TREATMENT OF HIV-1 INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	7176220	Aug. 27, 2026	TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	7635704	Oct. 26, 2026	TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	8148374	Sept. 3, 2029	TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	9891239	Sept. 3, 2029	TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	8633219	April 30, 2030	TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	8754065	Aug. 15, 2032	TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE	GENVOYA	GILEAD SCIENCES INC	N207561	Nov. 5, 2015	RX	TABLET	ORAL	9296769	Aug. 15, 2032	TREATMENT OF HIV INFECTION
150MG;800MG;200MG;EQ 10MG BASE	SYMTUZA	JANSSEN PRODS	N210455	July 17, 2018	RX	TABLET	ORAL	8148374	Sept. 3, 2029	TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
200MG;EQ 25MG BASE	DESCOVY	GILEAD SCIENCES INC	N208215	April 4, 2016	RX	TABLET	ORAL	Sept. 28, 2024	IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS, FOR THE TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS UNDER 12 YEARS OF AGE WEIGHING AT LEAST 35KG
200MG;EQ 25MG BASE	DESCOVY	GILEAD SCIENCES INC	N208215	April 4, 2016	RX	TABLET	ORAL	Sept. 28, 2024	IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS OTHER THAN PROTEASE INHIBITORS THAT REQUIRE A CYP3A INHIBITOR, FOR THE TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS UNDER 12 YEARS OF AGE WEIGHING AT LEAST 25KG AND LESS THAN 35KG
EQ 25MG BASE	VEMLIDY	GILEAD SCIENCES INC	N208464	Nov. 10, 2016	RX	TABLET	ORAL	Feb. 4, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY GS-US-320-4018 IN VIROLOGICALLY SUPPRESSED ADULTS W/ CHRONIC HEP B INFECTION WHO SWITCHED FROM TENOFOVIR DISOPROXIL FUMARATE TO TENOFOVIR ALAFENAMIDE
EQ 25MG BASE	VEMLIDY	GILEAD SCIENCES INC	N208464	Nov. 10, 2016	RX	TABLET	ORAL	Aug. 22, 2023	INFORMATION ADDED TO THE LABELING TO DESCRIBE STUDY GS-US-320-4035 IN VIROLOGICALLY SUPPRESSED ADULTS W/ CHRONIC HEP B INFECTION WHO SWITCHED FROM TENOFOVIR DISOPROXIL FUMARATE TO TENOFOVIR ALFAENAMIDE
EQ 25MG BASE	VEMLIDY	GILEAD SCIENCES INC	N208464	Nov. 10, 2016	RX	TABLET	ORAL	Oct. 17, 2025	NEW PATIENT POPULATION
EQ 30MG BASE;120MG;EQ 15MG BASE	BIKTARVY	GILEAD SCIENCES INC	N210251	Oct. 7, 2021	RX	TABLET	ORAL	Feb. 7, 2023	NEW CHEMICAL ENTITY
EQ 30MG BASE;120MG;EQ 15MG BASE	BIKTARVY	GILEAD SCIENCES INC	N210251	Oct. 7, 2021	RX	TABLET	ORAL	Oct. 7, 2028	A COMPLETE REGIMEN FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTS WEIGHING 14 KG TO LESS THAN 25 KG WHO HAVE NO ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY-SUPPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INDIVIDUAL COMPONENTS OF BIKTARVY
EQ 50MG BASE;200MG;EQ 25MG BASE	BIKTARVY	GILEAD SCIENCES INC	N210251	Feb. 7, 2018	RX	TABLET	ORAL	Feb. 7, 2023	NEW CHEMICAL ENTITY
EQ 50MG BASE;200MG;EQ 25MG BASE	BIKTARVY	GILEAD SCIENCES INC	N210251	Feb. 7, 2018	RX	TABLET	ORAL	Feb. 24, 2024	LABELING REVISIONS RELATED TO CLINICAL STUDIES
EQ 50MG BASE;200MG;EQ 25MG BASE	BIKTARVY	GILEAD SCIENCES INC	N210251	Feb. 7, 2018	RX	TABLET	ORAL	June 18, 2026	FOR HIV-1 INFECTION IN PEDIATRIC PTS AT LEAST 25 KG W/ NO ANTIRETROVIRAL (ARV) TX HX OR TO REPLACE CURRENT ARV REGIMEN FOR VIROLOGICALLY-SUPPRESSED ON STABLE ARV W/ NO HX TX FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED W/ RESISTANCE TO BIC, FTC, OR TAF

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Bioactivity Summary:

None

External reference:

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ID	Source
TFO	PDB_CHEM_ID
009357	NDDF
016564	NDDF
117466	RXNORM
1392275-56-7	SECONDARY_CAS_RN
206184-49-8	SECONDARY_CAS_RN
31269	MMSL
31575	MMSL
395264002	SNOMEDCT_US
4021279	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	50090-6247	TABLET	25 mg	ORAL	NDA	33 sections
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	61958-2501	TABLET	25 mg	ORAL	NDA	35 sections
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	61958-2501	TABLET	25 mg	ORAL	NDA	35 sections
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	61958-2505	TABLET	15 mg	ORAL	NDA	35 sections
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	61958-2505	TABLET	15 mg	ORAL	NDA	35 sections
Biktarvy	HUMAN PRESCRIPTION DRUG LABEL	3	70518-3080	TABLET	25 mg	ORAL	NDA	34 sections
DESCOVY	HUMAN PRESCRIPTION DRUG LABEL	2	61958-2002	TABLET	25 mg	ORAL	NDA	35 sections
DESCOVY	HUMAN PRESCRIPTION DRUG LABEL	2	61958-2005	TABLET	15 mg	ORAL	NDA	35 sections
DESCOVY	HUMAN PRESCRIPTION DRUG LABEL	2	70518-0230	TABLET	25 mg	ORAL	NDA	34 sections
Genvoya	HUMAN PRESCRIPTION DRUG LABEL	4	61958-1901	TABLET	10 mg	ORAL	NDA	32 sections

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