e-Drug3D

1805

TENOFOVIR ALAFENAMIDE


INN
TENOFOVIR ALAFENAMIDE

(has an active metabolite)

cas 379270-37-8
CLASS

ANTIINFECTIVES
TREATMENT OF HIV-1 INFECTION
CONVERTED IN VIVO TO TENOFOVIR

ROUTE (list)

ORAL

ATC code

J05AR17
J05AR20
J05AR29
J05AR19
J05AF13

PK parameters

Tmax 1 HOUR
Cmax 0.33 MICROMOLAR
PPB 80 PERCENT
t1/2 0.51 HOUR

Solubility

4.7 MILLIGRAM / MILLILITER


Target

TARGET HIV REVERSE TRANSCRIPTASE

DrugCentral

Reverse transcriptase,RNaseH UNIPROT Q72547 pol

Download SDF file L-Alanine, N-[(S)-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester

Formula:
C21H29N6O5P

Calculated chemical properties:

MW 476.47
NB_atoms 33
XLogP 2.97
PSA 134.7
NB_HD 3
NB_HA 11
fsp3 0.43
Lipinski(0=no;1=yes) 0

FDA
NDA 207561 (label) INN (COBICISTAT ; ELVITEGRAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) GENVOYA (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2015
NDA 208215 (label) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) DESCOVY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2016
NDA 208351 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR ALAFENAMIDE FUMARATE) ODEFSEY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2016
NDA 208464 (label) INN (TENOFOVIR ALAFENAMIDE FUMARATE) VEMLIDY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2016
NDA 210251 (label) INN (BICTEGRAVIR SODIUM ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) BIKTARVY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2018
NDA 210455 (label) INN (COBICISTAT ; DARUNAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) SYMTUZA (JANSSEN PRODS) APPROVAL= AP YEAR= 2018
NDA 213845 (pdf not found) INN (TENOFOVIR ALAFENAMIDE) TENOFOVIR ALAFENAMIDE (SUNSHINE LAKE) APPROVAL= TA YEAR= 2021
NDA 212527 (pdf not found) INN (DOLUTEGRAVIR ; LAMIVUDINE ; TENOFOVIR ALAFENAMIDE) DOLUTEGRAVIR LAMIVUDINE TENOFOVIR ALAFENAMIDE (CIPLA USA INC.) APPROVAL= TA YEAR= 2022
NDA 214058 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE (CIPLA LIMITED) APPROVAL= TA YEAR= 2022
NDA 214072 (pdf not found) INN (TENOFOVIR ALAFENAMIDE) TENOFOVIR ALAFENAMIDE (SHILPA MEDICARE LTD) APPROVAL= TA YEAR= 2022
NDA 216875 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; TENOFOVIR ALAFENAMIDE (AUROBINDO PHARMA) APPROVAL= TA YEAR= 2022
NDA 214226 (pdf not found) INN (TENOFOVIR ALAFENAMIDE FUMARATE) TENOFOVIR ALAFENAMIDE (LUPIN) APPROVAL= AP YEAR= 2023
NDA 214544 (pdf not found) INN (DOLUTEGRAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) DOLUTEGRAVIR; EMTRICITABINE; TENOFOVIR ALAFENAMIDE (LUPIN LTD) APPROVAL= TA YEAR= 2023
NDA 215448 (pdf not found) INN (DOLUTEGRAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) DOLUTEGRAVIR, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (AUROBINDO PHARMA USA) APPROVAL= TA YEAR= 2023
NDA 215187 (pdf not found) INN (DOLUTEGRAVIR ; LAMIVUDINE ; TENOFOVIR ALAFENAMIDE) DOLUTEGRAVIR;LAMIVUDINE;TENOFOVIR ALAFENAMIDE (LUPIN PHARMS) APPROVAL= TA YEAR= 2023
NDA 211148 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (MYLAN LABS LTD) APPROVAL= TA YEAR= 2024
NDA 213509 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EFAVIRENZ, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (MYLAN) APPROVAL= TA YEAR= 2024
NDA 213867 (pdf not found) INN (TENOFOVIR ALAFENAMIDE FUMARATE) TENOFOVIR ALAFENAMIDE FUMARATE (APOTEX) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 214053 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FUMARATE (APOTEX) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 213926 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FUMARATE (LUPIN) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 215071 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; TENOFOVIR ALAFENAMIDE (LUPIN LTD) APPROVAL= TA YEAR= 2024
NDA 216914 (pdf not found) INN (BICTEGRAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) BICTEGRAVIR, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (CIPLA LTD) APPROVAL= TA YEAR= 2025
NDA 211680 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (CIPLA LIMITED) APPROVAL= TA YEAR= 2025
NDA 218766 (pdf not found) INN (BICTEGRAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) BICTEGRAVIR, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (CIPLA LTD) APPROVAL= TA YEAR= 2025
NDA 214030 (pdf not found) INN (TENOFOVIR ALAFENAMIDE FUMARATE) TENOFOVIR ALAFENAMIDE FUMARATE (LAURUS LABS LTD) APPROVAL= TA YEAR= 2026
NDA 214095 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE, RILPIVIRINE, AND TENOFOVIR ALAFENAMIDE (APOTEX) APPROVAL= AP YEAR= 2026
NDA 214216 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FUMARATE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2026
NDA 218575 (pdf not found) INN (ELVITEGRAVIR ; COBICISTAT ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) ELVITEGRAVIR, COBICISTAT, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE (APOTEX INC) APPROVAL= TA YEAR= 2026

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1491

TENOFOVIR


INN
TENOFOVIR

(is an active metabolite)

cas 147127-20-6
CLASS

ANTIINFECTIVE
ANTIVIRAL
ANTIRETROVIRAL
NUCLEOTIDE ANALOG HIV-1 REVERSE TRANSCRIPTASE INHIBITOR AND
HBV REVERSE TRANSCRIPTASE INHIBITOR
CHRONIC HEPATITIS B IN ADULTS

ROUTE (list)

-

ATC code

J05AR06
J05AR08
J05AR12
J05AR27
J05AR24
J05AR11
J05AF07
J05AR03

PK parameters

F 25 PERCENT
Cmax 0.578 MICROMOLAR (300 MILLIGRAM)
VD 84.5 LITER (65 KILOGRAM)
Cl 3.4 LITER / HOUR (EQN)
PPB 7 PERCENT
t1/2 17 HOUR

Target

TARGET HIV REVERSE TRANSCRIPTASE

PDB
8BVS (CRYO-EM STRUCTURE OF RAT SLC22A6 BOUND TO TENOFOVIR)

Ligand code = TFO (link to the list of PDB complexes)

Download experimental 3D coordinates of TFO with added hydrogens

DrugCentral

Reverse transcriptase,RNaseH UNIPROT Q72547 pol

Download SDF file [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid

Formula:
C9H14N5O4P

Calculated chemical properties:

MW 285.21
NB_atoms 19
XLogP -1.32
PSA 124.294
NB_HD 2
NB_HA 9
fsp3 0.44
Lipinski(0=no;1=yes) 1

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL