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EMTRICITABINE


INN
EMTRICITABINE

cas 143491-57-0
CLASS

ANTIINFECTIVES
ANTIVIRAL
HIV-1 REVERSE TRANSCRIPTASE INHIBITOR

ROUTE (list)

ORAL

ATC code

J05AF09
J05AR17
J05AR20
J05AR29
J05AR19
J05AR22
J05AR18
J05AR06
J05AR08
J05AR09
J05AR03

PK parameters

F 75 PERCENT
Tmax 1.5 HOUR
VD 91 LITER (65 KILOGRAM)
Cl 18.1 LITER / HOUR
PPB 4 PERCENT
t1/2 10 HOUR

Solubility

112 MILLIGRAM / MILLILITER IN WATER


Target

TARGET HIV-1 REVERSE TRANSCRIPTASE

PDB
2NO6 (C4S DCK VARIANT OF DCK IN COMPLEX WITH FTC+ADP)

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

Download experimental 3D coordinates of ETV with added hydrogens

DrugCentral

Reverse transcriptase,RNaseH UNIPROT Q72547 pol

Download SDF file 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one

Formula:
C8H10FN3O3S

Calculated chemical properties:

MW 247.26
NB_atoms 16
XLogP -0.46
PSA 82.926
NB_HD 3
NB_HA 6
fsp3 0.50
Lipinski(0=no;1=yes) 1

FDA
NDA 021500 (label) INN (EMTRICITABINE) EMTRIVA (GILEAD) APPROVAL= AP YEAR= 2003 NEWMOLECULARENTITY
NDA 021752 (label) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) TRUVADA (GILEAD) APPROVAL= AP YEAR= 2004
NDA 021896 (label) INN (EMTRICITABINE) EMTRIVA (GILEAD) APPROVAL= AP YEAR= 2005
NDA 021937 (label) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) ATRIPLA (GILEAD SCIENCES) APPROVAL= AP YEAR= 2006
NDA 090488 (pdf not found) INN (EMTRICITABINE) EMTRICITABINE (MATRIX LABS LTD) APPROVAL= TA YEAR= 2008
NDA 090049 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE (MATRIX LABS LTD) APPROVAL= TA YEAR= 2009
NDA 090437 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ; EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE (MATRIX LABS LTD) APPROVAL= TA YEAR= 2009
NDA 202123 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR DISOPROXIL FUMARATE) COMPLERA (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2011
NDA 091593 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ; EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE (CIPLA LIMITED) APPROVAL= TA YEAR= 2012
NDA 203100 (label) INN (COBICISTAT ; ELVITEGRAVIR ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) STRIBILD (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2012
NDA 206042 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE ; NEVIRAPINE) EMTRICITABINE;TENOFOVIR DISOPROXIL FUMARATE;NEVIRAPINE (MYLAN LABS LTD) APPROVAL= TA YEAR= 2014
NDA 206584 (pdf not found) INN (EMTRICITABINE) EFAVIRENZ; EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE (EMCURE PHARMS LTD) APPROVAL= TA YEAR= 2015 OBSOLETE
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 090894 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2017
NDA 208452 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE;RILPIVIRINE;TENOFOVIR DISOPROXIL FUMARATE (MYLAN PHARMS INC) APPROVAL= TA YEAR= 2017
NDA 090513 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2018
NDA 091168 (pdf not found) INN (EMTRICITABINE) EMTRICITABINE (CIPLA) APPROVAL= AP YEAR= 2018
NDA 091215 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (TEVA PHARMS USA) APPROVAL= AP YEAR= 2018
NDA 203041 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2018
NDA 206436 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (MYLAN) APPROVAL= AP YEAR= 2018
NDA 210251 (label) INN (BICTEGRAVIR SODIUM ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) BIKTARVY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2018
NDA 209721 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (AMNEAL PHARMS CO) APPROVAL= AP YEAR= 2018
NDA 210455 (label) INN (COBICISTAT ; DARUNAVIR ; EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) SYMTUZA (JANSSEN PRODS) APPROVAL= AP YEAR= 2018
NDA 206894 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (CIPLA) APPROVAL= AP YEAR= 2019
NDA 212114 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (LAURUS) APPROVAL= AP YEAR= 2019
NDA 203442 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2020
NDA 212689 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2020
NDA 201806 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2021
NDA 091055 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (STRIDES PHARMA) APPROVAL= AP YEAR= 2021
NDA 090958 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (CIPLA) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 204287 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2021
NDA 204131 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (CHARTWELL RX) APPROVAL= AP YEAR= 2021
NDA 208740 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (APOTEX) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 213541 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (LAURUS) APPROVAL= AP YEAR= 2021
NDA 203053 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2022
NDA 214058 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE (CIPLA LIMITED) APPROVAL= TA YEAR= 2022
NDA 216875 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; TENOFOVIR ALAFENAMIDE (AUROBINDO PHARMA) APPROVAL= TA YEAR= 2022
NDA 079188 (pdf not found) INN (EMTRICITABINE) EMTRICITABINE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023
NDA 211640 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (AUROBINDO PHARMA LTD) 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 201802 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ; EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE (STRIDES PHARMA) APPROVAL= AP 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 214053 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FUMARATE (APOTEX) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 209061 (pdf not found) INN (EFAVIRENZ ; EMTRICITABINE ; TENOFOVIR DISOPROXIL FUMARATE) EFAVIRENZ; EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE (MYLAN) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 213926 (pdf not found) INN (EMTRICITABINE ; TENOFOVIR ALAFENAMIDE FUMARATE) EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FUMARATE (LUPIN LTD) APPROVAL= AP YEAR= 2024
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

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL