e-Drug3D

865

cas 100643-71-8

CLASS

RESPIRATORY
HISTAMINE H1 RECEPTOR ANTAGONIST
ANTIHISTAMINE
CHOLINERGIC ANTAGONISTS

ROUTE (list)

ORAL

PK parameters

Tmax 3 HOUR
Cmax 12.8 NANOMOLAR
PPB 84 PERCENT
t1/2 27 HOUR

TARGET HISTAMINE H1 RECEPTOR

PDB
8X64 (CRYOEM STRUCTURE OF THE HISTAMINE H1 RECEPTOR-BRIL, ANTI BRIL FAB COMPLEX WITH DESLORATADINE)

Ligand code = Y5R (link to the list of PDB complexes)

Download experimental 3D coordinates of Y5R with added hydrogens

MW 310.81
NB_atoms 22
XLogP 4.02
PSA 21.772
NB_HD 1
NB_HA 2
fsp3 0.32
Lipinski(0=no;1=yes) 1

FDA
NDA 021165 (label) INN (DESLORATADINE) CLARINEX (ORGANON) APPROVAL= AP YEAR= 2001 NEWMOLECULARENTITY
NDA 021297 (label) INN (DESLORATADINE) CLARINEX (SCHERING) APPROVAL= AP YEAR= 2002 NEWAPPLICATION
NDA 021312 (label) INN (DESLORATADINE) CLARINEX (ORGANON) APPROVAL= AP YEAR= 2002 DISCONTINUED
NDA 021363 (label) INN (DESLORATADINE) CLARINEX (SCHERING) APPROVAL= AP YEAR= 2002 NEWAPPLICATION
NDA 021300 (label) INN (DESLORATADINE) CLARINEX (ORGANON LLC) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 021563 (label) INN (DESLORATADINE) CLARINEX (SCHERING) APPROVAL= AP YEAR= 2004
NDA 021605 (label) INN (DESLORATADINE ; PSEUDOEPHEDRINE SULFATE) CLARINEX D 24 HOUR (ORGANON) APPROVAL= AP YEAR= 2005 DISCONTINUED
NDA 021313 (label) INN (DESLORATADINE ; PSEUDOEPHEDRINE SULFATE) CLARINEX-D 12 HOUR (ORGANON LLC) APPROVAL= AP YEAR= 2006
NDA 078362 (pdf not found) INN (DESLORATADINE) DESLORATADINE (GLENMARK GENERICS) APPROVAL= TA YEAR= 2009
NDA 078357 (pdf not found) INN (DESLORATADINE) DESLORATADINE (ORBION PHARMS) APPROVAL= AP YEAR= 2010
NDA 078352 (pdf not found) INN (DESLORATADINE) DESLORATADINE (LUPIN PHARMS) APPROVAL= AP YEAR= 2010
NDA 078359 (pdf not found) INN (DESLORATADINE) DESLORATADINE (SUN PHARM INDS) APPROVAL= AP YEAR= 2010 DISCONTINUED
NDA 078367 (pdf not found) INN (DESLORATADINE) DESLORATADINE (REDDYS) APPROVAL= AP YEAR= 2010
NDA 078364 (pdf not found) INN (DESLORATADINE) DESLORATADINE (CHARTWELL RX) APPROVAL= AP YEAR= 2010 DISCONTINUED
NDA 078353 (pdf not found) INN (DESLORATADINE) DESLORATADINE (ZYDUS PHARMS USA) APPROVAL= TA YEAR= 2011
NDA 078365 (pdf not found) INN (DESLORATADINE) DESLORATADINE (DR REDDYS LABS LTD) APPROVAL= AP YEAR= 2011
NDA 078366 (pdf not found) INN (DESLORATADINE ; PSEUDOEPHEDRINE SULFATE) DESLORATADINE AND PSEUDOEPHEDRINE SULFATE 24 HOUR (DR REDDYS LABS LTD) APPROVAL= AP YEAR= 2011
NDA 078361 (pdf not found) INN (DESLORATADINE) DESLORATADINE (PERRIGO) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 078351 (pdf not found) INN (DESLORATADINE) DESLORATADINE (NATCO PHARMA USA) APPROVAL= AP YEAR= 2012
NDA 078355 (pdf not found) INN (DESLORATADINE) DESLORATADINE (AJENAT PHARMS) APPROVAL= AP YEAR= 2012
NDA 202592 (pdf not found) INN (DESLORATADINE) DESLORATADINE (TARO) APPROVAL= AP YEAR= 2015 DISCONTINUED
NDA 202936 (pdf not found) INN (DESLORATADINE) DESLORATADINE (TARO) APPROVAL= AP YEAR= 2016

e-Drug3D

621

cas 79794-75-5

CLASS

RESPIRATORY SYSTEM
ANTIHISTAMINE
ANTI-ALLERGIC AGENTS
ANTIPRURITICS
HISTAMINE H1 ANTAGONISTS, NON-SEDATING

ROUTE (list)

ORAL

PK parameters

Tmax 1.3 HOUR
Cmax 10 NANOMOLAR (PMID18621671)
PPB 98 PERCENT
t1/2 8.4 HOUR

MW 382.87
NB_atoms 27
XLogP 4.89
PSA 35.3
NB_HD 0
NB_HA 4
fsp3 0.36
Lipinski(0=no;1=yes) 1

FDA
NDA 019658 (label) INN (LORATADINE) CLARITIN (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 1993
NDA 019670 (label) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) CLARITIN-D (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 1994
NDA 020470 (label) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) CLARITIN-D 24 HOUR (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 1996
NDA 020641 (label) INN (LORATADINE) CLARITIN (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 1996
NDA 020704 (label) INN (LORATADINE) CLARITIN REDITABS (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 1996
NDA 021375 (label) INN (LORATADINE) ALAVERT (FDN CONSUMER) APPROVAL= AP YEAR= 2002
NDA 076127 (pdf not found) INN (LORATADINE) LORATADINE (TARO) APPROVAL= TA YEAR= 2002 OBSOLETE
NDA 075209 (pdf not found) INN (LORATADINE) LORATADINE (PLD ACQUISITIONS LLC) APPROVAL= AP YEAR= 2003
NDA 075505 (pdf not found) INN (LORATADINE) LORATADINE (TEVA) APPROVAL= AP YEAR= 2003 DISCONTINUED
NDA 075706 (label) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (P AND L) APPROVAL= AP YEAR= 2003
NDA 075822 (pdf not found) INN (LORATADINE) LORATADINE (GLAXOSMITHKLINE) APPROVAL= AP YEAR= 2003 DISCONTINUED
NDA 075990 (pdf not found) INN (LORATADINE) LORATADINE (ACTAVIS LABS FL INC) APPROVAL= AP YEAR= 2003 DISCONTINUED
NDA 076011 (pdf not found) INN (LORATADINE) LORATADINE (PERRIGO PHARMA INTL) APPROVAL= AP YEAR= 2003
NDA 076050 (pdf not found) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (PERRIGO PHARMA INTL) APPROVAL= AP YEAR= 2003
NDA 076134 (pdf not found) INN (LORATADINE) LORATADINE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2003
NDA 076154 (pdf not found) INN (LORATADINE) LORATADINE (MYLAN) APPROVAL= AP YEAR= 2003
NDA 021512 (label) INN (LORATADINE) LORATADINE (PERRIGO) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 075565 (pdf not found) INN (LORATADINE) LORATADINE (PHARM ASSOC) APPROVAL= AP YEAR= 2004
NDA 075728 (pdf not found) INN (LORATADINE) LORATADINE (PERRIGO) APPROVAL= AP YEAR= 2004
NDA 075815 (pdf not found) INN (LORATADINE) LORATADINE (WOCKHARDT BIO AG) APPROVAL= AP YEAR= 2004
NDA 075989 (pdf not found) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (PERRIGO PHARMA INTL) APPROVAL= AP YEAR= 2004
NDA 076208 (pdf not found) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (HERITAGE PHARMA) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 076301 (pdf not found) INN (LORATADINE) LORATADINE (PERRIGO) APPROVAL= AP YEAR= 2004
NDA 076529 (pdf not found) INN (LORATADINE) LORATADINE (RANBAXY LABS LTD) APPROVAL= AP YEAR= 2004 DISCONTINUED
NDA 076557 (pdf not found) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2004
NDA 076805 (pdf not found) INN (LORATADINE) LORATADINE (TARO) APPROVAL= AP YEAR= 2004
NDA 021734 (label) INN (LORATADINE) LORATADINE (SUN PHARMA CANADA) APPROVAL= AP YEAR= 2005 DISCONTINUED
NDA 021891 (label) INN (LORATADINE) CHILDREN'S CLARITIN (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 2006
NDA 021993 (label) INN (LORATADINE) CLARITIN REDITABS (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 2006
NDA 076471 (pdf not found) INN (LORATADINE) LORATADINE (APOTEX) APPROVAL= AP YEAR= 2006
NDA 077421 (pdf not found) INN (LORATADINE) LORATADINE (LANNETT CO INC) APPROVAL= AP YEAR= 2006
NDA 077153 (pdf not found) INN (LORATADINE) LORATADINE REDIDOSE (SUN PHARM INDS LTD) APPROVAL= AP YEAR= 2007
NDA 021952 (label) INN (LORATADINE) CLARITIN (BAYER HEALTHCARE LLC) APPROVAL= AP YEAR= 2008
NDA 075790 (pdf not found) INN (LORATADINE) LORATADINE (PHARMOBEDIENT) APPROVAL= AP YEAR= 2008 DISCONTINUED
NDA 078447 (pdf not found) INN (LORATADINE) LORATADINE (PHARMOBEDIENT) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 201865 (pdf not found) INN (LORATADINE) LORATADINE (TARO) APPROVAL= AP YEAR= 2015
NDA 206214 (label) INN (LORATADINE) LORATADINE (MARKSANS PHARMA) APPROVAL= AP YEAR= 2016
NDA 208314 (pdf not found) INN (LORATADINE) LORATADINE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2018
NDA 208477 (label) INN (LORATADINE) LORATADINE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2018
NDA 210088 (pdf not found) INN (LORATADINE) LORATADINE (SUN PHARM) APPROVAL= AP YEAR= 2018
NDA 202538 (pdf not found) INN (LORATADINE) LORATADINE (BIONPHARMA) APPROVAL= AP YEAR= 2018
NDA 208931 (pdf not found) INN (LORATADINE) LORATADINE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2018
NDA 207569 (pdf not found) INN (LORATADINE) LORATADINE (ANDA REPOSITORY) APPROVAL= AP YEAR= 2019
NDA 210033 (pdf not found) INN (LORATADINE) LORATADINE (PERRIGO PHARMA INTL) APPROVAL= AP YEAR= 2019
NDA 210722 (pdf not found) INN (LORATADINE) LORATADINE (GRANULES) APPROVAL= AP YEAR= 2019
NDA 211926 (pdf not found) INN (LORATADINE) LORATADINE (ONESOURCE SPECIALTY) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 212795 (pdf not found) INN (LORATADINE) LORATADINE (INSTAPILL) APPROVAL= AP YEAR= 2020
NDA 213294 (pdf not found) INN (LORATADINE) LORATADINE (INSTAPILL) APPROVAL= AP YEAR= 2020
NDA 214280 (pdf not found) INN (LORATADINE) LORATADINE (RUBICON RESEARCH) APPROVAL= AP YEAR= 2020
NDA 210409 (pdf not found) INN (LORATADINE) LORATADINE (HETERO LABS LTD III) APPROVAL= AP YEAR= 2021
NDA 214684 (pdf not found) INN (LORATADINE) LORATADINE (UNIQUE PHARM) APPROVAL= AP YEAR= 2021
NDA 211900 (pdf not found) INN (LORATADINE) LORATADINE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2023
NDA 211718 (pdf not found) INN (LORATADINE) LORATADINE (HETERO LABS LTD V) APPROVAL= AP YEAR= 2023
NDA 218017 (pdf not found) INN (LORATADINE ; PSEUDOEPHEDRINE SULFATE) LORATADINE AND PSEUDOEPHEDRINE SULFATE (BIONPHARMA) APPROVAL= AP YEAR= 2024
NDA 219223 (pdf not found) INN (LORATADINE) LORATADINE (MARKSANS PHARMA) APPROVAL= AP YEAR= 2024
NDA 215127 (pdf not found) INN (LORATADINE) LORATADINE (CATALENT PHARMA) APPROVAL= AP YEAR= 2025 DISCONTINUED