e-Drug3D
1516
RILPIVIRINE
INN
RILPIVIRINE
cas 500287-72-9
CLASS
ANTIINFECTIVES
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (NNRTI) OF HIV-1
ROUTE (list)
ORAL INTRAMUSCULAR
PK parameters
Tmax 4.5 HOUR
PPB 99.7 PERCENT
t1/2 50 HOUR
Solubility
PRACTICALLY INSOLUBLE IN WATER OVER A WIDE PH RANGE
TARGET HIV-1 REVERSE TRANSCRIPTASE (EC50(HIV-1IIIB) = 0.73 NM)
PDB
2ZE2 (CRYSTAL STRUCTURE OF L100I, K103N MUTANT HIV-1 REVERSE TRANSCRIPTASE (RT) IN COMPLEX WITH TMC278 (RILPIVIRINE), A NON-NUCLEOSIDE RT INHIBITOR)
Ligand code = T27 (link to the list of PDB complexes)
Download experimental 3D coordinates of T27 with added hydrogens
Reverse transcriptase,RNaseH UNIPROT Q72547 pol
Formula:
C22H18N6
Calculated chemical properties:
MW 366.42
NB_atoms 28
XLogP 4.99
PSA 79.076
NB_HD 2
NB_HA 6
fsp3 0.09
Lipinski(0=no;1=yes) 1
NB_atoms 28
XLogP 4.99
PSA 79.076
NB_HD 2
NB_HA 6
fsp3 0.09
Lipinski(0=no;1=yes) 1
FDA
NDA 202022 (label) INN (RILPIVIRINE HYDROCHLORIDE) EDURANT (JANSSEN PRODS) APPROVAL= AP YEAR= 2011 NEWMOLECULARENTITY
NDA 202123 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR DISOPROXIL FUMARATE) COMPLERA (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2011
NDA 205302 (pdf not found) INN (RILPIVIRINE) RILPIVIRINE (STRIDES ARCOLAB LTD) APPROVAL= TA YEAR= 2015
NDA 208351 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR ALAFENAMIDE FUMARATE) ODEFSEY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2016
NDA 208452 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE;RILPIVIRINE;TENOFOVIR DISOPROXIL FUMARATE (MYLAN PHARMS INC) APPROVAL= TA YEAR= 2017
NDA 210192 (label) INN (DOLUTEGRAVIR SODIUM ; RILPIVIRINE HYDROCHLORIDE) JULUCA (VIIV HLTHCARE) APPROVAL= AP YEAR= 2017
NDA 212888 (label) INN (CABOTEGRAVIR ; RILPIVIRINE) CABENUVA KIT (VIIV HLTHCARE) APPROVAL= AP YEAR= 2021
NDA 214058 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE (CIPLA LIMITED) APPROVAL= TA YEAR= 2022
NDA 213120 (pdf not found) INN (DOLUTEGRAVIR ; RILPIVIRINE) DOLUTEGRAVIR; RILPIVIRINE (LUPIN LTD) APPROVAL= TA YEAR= 2023
NDA 219016 (label) INN (RILPIVIRINE HYDROCHLORIDE) EDURANT PED (JANSSEN PRODS) APPROVAL= AP YEAR= 2024
NDA 218798 (pdf not found) INN (RILPIVIRINE) RILPIVIRINE (SOMERSET THERAPEUTICS, LLC) APPROVAL= TA YEAR= 2025
NDA 202022 (label) INN (RILPIVIRINE HYDROCHLORIDE) EDURANT (JANSSEN PRODS) APPROVAL= AP YEAR= 2011 NEWMOLECULARENTITY
NDA 202123 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR DISOPROXIL FUMARATE) COMPLERA (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2011
NDA 205302 (pdf not found) INN (RILPIVIRINE) RILPIVIRINE (STRIDES ARCOLAB LTD) APPROVAL= TA YEAR= 2015
NDA 208351 (label) INN (EMTRICITABINE ; RILPIVIRINE HYDROCHLORIDE ; TENOFOVIR ALAFENAMIDE FUMARATE) ODEFSEY (GILEAD SCIENCES INC) APPROVAL= AP YEAR= 2016
NDA 208452 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR DISOPROXIL FUMARATE) EMTRICITABINE;RILPIVIRINE;TENOFOVIR DISOPROXIL FUMARATE (MYLAN PHARMS INC) APPROVAL= TA YEAR= 2017
NDA 210192 (label) INN (DOLUTEGRAVIR SODIUM ; RILPIVIRINE HYDROCHLORIDE) JULUCA (VIIV HLTHCARE) APPROVAL= AP YEAR= 2017
NDA 212888 (label) INN (CABOTEGRAVIR ; RILPIVIRINE) CABENUVA KIT (VIIV HLTHCARE) APPROVAL= AP YEAR= 2021
NDA 214058 (pdf not found) INN (EMTRICITABINE ; RILPIVIRINE ; TENOFOVIR ALAFENAMIDE) EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE (CIPLA LIMITED) APPROVAL= TA YEAR= 2022
NDA 213120 (pdf not found) INN (DOLUTEGRAVIR ; RILPIVIRINE) DOLUTEGRAVIR; RILPIVIRINE (LUPIN LTD) APPROVAL= TA YEAR= 2023
NDA 219016 (label) INN (RILPIVIRINE HYDROCHLORIDE) EDURANT PED (JANSSEN PRODS) APPROVAL= AP YEAR= 2024
NDA 218798 (pdf not found) INN (RILPIVIRINE) RILPIVIRINE (SOMERSET THERAPEUTICS, LLC) APPROVAL= TA YEAR= 2025