RUPATADINE FUMARATE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C26H26ClN3.C4H4O4
Molecular Weight	532.03
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C\C(O)=O.CC1=CN=CC(CN2CCC(CC2)=C3C4=CC=C(Cl)C=C4CCC5=CC=CN=C35)=C1

InChI

InChIKey=JYBLCDXVHQWMSU-WLHGVMLRSA-N

InChI=1S/C26H26ClN3.C4H4O4/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25;5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+

HIDE SMILES / InChI

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Molecular Formula	C26H26ClN3
Molecular Weight	415.958
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.tga.gov.au/auspar/auspar-rupatadine
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8996188 | https://www.ncbi.nlm.nih.gov/pubmed/27500993

Rupatadine is characterised as a non-sedating H1 anti-histamine and platelet-activating factor (PAF) receptor antagonist. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 316 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996188 \| https://www.ncbi.nlm.nih.gov/pubmed/27500993 \| https://www.tga.gov.au/auspar/auspar-rupatadine	Antagonist 2849
Platelet activating factor receptor 20 Target ID: CHEMBL250 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996188 \| https://www.ncbi.nlm.nih.gov/pubmed/27500993 \| https://www.tga.gov.au/auspar/auspar-rupatadine	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Allergic rhinitis 104 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17020424 https://www.ncbi.nlm.nih.gov/pubmed/27500993	Primary		Approved 8583	RUPAFIN Approved Use Symptomatic treatment of allergic rhinitis and urticaria Launch Date 2002
Urticaria 39 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17020424 https://www.ncbi.nlm.nih.gov/pubmed/27500993	Primary		Approved 8583	RUPAFIN Approved Use Symptomatic treatment of allergic rhinitis and urticaria Launch Date 2002

C_max

Value	Dose	Analyte	Population
4.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
3.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
4.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
81.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
35.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.34 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.43 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.91 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
16.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
50.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
47.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
15.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
27.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
35.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
60.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
75.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
29.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
32.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
49.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
57.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
117.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
132.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
214.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
296.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
198.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
399.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.47 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
30.66 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.86 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.66 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
0.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT
1.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
4.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
24.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
24.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=25	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
13.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
11 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RUPATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=26 \| https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_K101_1.pdf#page=95	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESLORATADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.9% OTHER GOV'T https://www.pmda.go.jp/drugs/2017/P20170830003/470006000_22900AMX00962_A100_1.pdf#page=13			RUPATADINE plasma	Homo sapiens

Doses

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral Higher than recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27632557/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27632557/	Sources: https://pubmed.ncbi.nlm.nih.gov/27632557/
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20406224/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20406224/	Other AEs: Somnolence... Other AEs: Somnolence (53.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/20406224/
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30391169/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30391169/	Sources: https://pubmed.ncbi.nlm.nih.gov/30391169/

AEs

AE	Significance	Dose	Population
Somnolence	53.7%	100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20406224/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20406224/

PubMed

Title	Date	PubMed
Efficacy and tolerability of rupatadine at four times the recommended dose against histamine- and platelet-activating factor-induced flare responses and ex vivo platelet aggregation in healthy males.	2010-12	20819087
Rupatadine and levocetirizine for seasonal allergic rhinitis: a comparative study of efficacy and safety.	2010-08	20713756
Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double-blind, crossover, repeated dose, placebo-controlled study.	2010-06	20565458
Rupatadine improves nasal symptoms, airflow and inflammation in patients with persistent allergic rhinitis: a pilot study.	2010-05-22	20487631
No cardiac effects of therapeutic and supratherapeutic doses of rupatadine: results from a 'thorough QT/QTc study' performed according to ICH guidelines.	2010-04	20406224
[Rupatadine, oral Rupatall].	2010-03	20429393
Stereoselective synthesis of desloratadine derivatives as antagonist of histamine.	2010-02-15	20110173
Rupatadine and its effects on symptom control, stimulation time, and temperature thresholds in patients with acquired cold urticaria.	2010-01	20143651
Rupatadine and heart rhythm disturbances.	2010-01	19727070
Structurally diverse metal coordination compounds, bearing imidodiphosphinate and diphosphinoamine ligands, as potential inhibitors of the platelet activating factor.	2010	20689709
Rupatadine inhibits proinflammatory mediator secretion from human mast cells triggered by different stimuli.	2010	19672095
Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis.	2009-12	23120659
Paradoxical exacerbation of chronic urticaria by H1-antihistamines and montelukast.	2009-12	20128233
The use of a responder analysis to identify clinically meaningful differences in chronic urticaria patients following placebo- controlled treatment with rupatadine 10 and 20 mg.	2009-09	19453774
Treatment of acquired cold urticaria with rupatadine.	2009-09	19392988
Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines.	2009-08-31	21437146
Unsuspected polymorphic metabolism of rupatadine via its primary metabolite, desloratadine.	2009-06	19172210
Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis.	2009-06	18695846
Heart rhythm disturbances associated with rupatadine: a case series from the Spanish and Portuguese pharmacovigilance systems.	2009-05	19225450
Torsade de pointes associated with rupatadine.	2009-03	19268083
Simultaneous determination of rupatadine and its metabolite desloratadine in human plasma by a sensitive LC-MS/MS method: application to the pharmacokinetic study in healthy Chinese volunteers.	2009-02-20	19059745
Successful treatment of chronic drug-resistant urticaria with alprazolam.	2009-02	19203665
Reduction of nasal volume after allergen-induced rhinitis in patients treated with rupatadine: a randomized, cross-over, double-blind, placebo-controlled study.	2009	20128424
Safety of rupatadine administered over a period of 1 year in the treatment of persistent allergic rhinitis: a multicentre, open-label study in Spain.	2009	19132803
Antihistaminic effects of rupatadine and PKPD modelling.	2008-09-10	18777946
Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.	2008-09	18840369
Herbex-kid Inhibits Immediate Hypersensitivity Reactions in Mice and Rats.	2008-09	18830458
Determination of rupatadine in pharmaceutical formulations by a validated stability-indicating MEKC method.	2008-09	18693320
High performance liquid chromatography-tandem mass spectrometric determination of rupatadine in human plasma and its pharmacokinetics.	2008-08-05	18472381
A 12-week placebo-controlled study of rupatadine 10 mg once daily compared with cetirizine 10 mg once daily, in the treatment of persistent allergic rhinitis.	2008-07	18588560
Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis.	2008-05-27	19893935
Rupatadine in allergic rhinitis and chronic urticaria.	2008-04	18339040
[Torsades de pointes associated with rupatadine].	2008-03	18361911
Lack of effects between rupatadine 10 mg and placebo on actual driving performance of healthy volunteers.	2007-07	17599335
Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study.	2007-05	17697908
Rupatadine in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled multicentre study.	2007-05	17441794
[Protective effect of rupatadine against oleic acid-induced acute lung injury in rabbits].	2007-03	17520822
[Antihistamines in allergic rhinitis].	2007	18260244
Characterization of the de novo biosynthetic enzyme of platelet activating factor, DDT-insensitive cholinephosphotransferase, of human mesangial cells.	2007	17710109
Rupatadine: a review of its use in the management of allergic disorders.	2007	17335300
The proarrhythmic antihistaminic drug terfenadine increases spontaneous calcium release in human atrial myocytes.	2006-12-28	17078945
Once-daily rupatadine improves the symptoms of chronic idiopathic urticaria: a randomised, double-blind, placebo-controlled study.	2006-12-22	17478385
New antihistamines: a critical view.	2006-11	17136293
Rupatadine: pharmacological profile and its use in the treatment of allergic disorders.	2006-10	17020424
Effects of rupatadine vs placebo on allergen-induced symptoms in patients exposed to aeroallergens in the Vienna Challenge Chamber.	2006-01	16440531
Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers.	2006-01	16389668
Rupatadine 10 mg and cetirizine 10 mg in seasonal allergic rhinitis: a randomised, double-blind parallel study.	2005	15864879
Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study.	2004-07	15180765
Central and peripheral evaluation of rupatadine, a new antihistamine/platelet-activating factor antagonist, at different doses in healthy volunteers.	2004	15539863
A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis.	2004	15160440

Patents

Sample Use Guides

In Vivo Use Guide

Adults and adolescents (over 12 years of age): The recommended dose is 10 mg (one tablet) once a day, with or without food. Paediatric patients: Rupatadine 10 mg Tablets is not recommended for use in children below age 12. In children aged 2 to 11 years, the administration of rupatadine 1 mg/ml oral solution is recommended.

Route of Administration: Oral

In Vitro Use Guide

platelet-activating factor stimulated a statistically significant release of histamine, interleukin-8, and tumor necrosis factor (0.001-0.1 μmol/L). Pretreatment with rupatadine (25 μmol/L) for 10 minutes inhibited this effect.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:07:45 GMT 2025` Edited by `admin` on `Mon Mar 31 19:07:45 GMT 2025`
Record UNII	XJ6OT32M93
Record Status	`Validated (UNII)`
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Name

Type

Language

RUPAFIN

Preferred Name

English

RUPATADINE FUMARATE

Common Name

English

RUPATADINE FUMARATE [MI]

Common Name

English

Rupatadine fumarate [WHO-DD]

Common Name

English

RUPATADINE FUMARATE [JAN]

Common Name

English

5H-BENZO(5,6)CYCLOHEPTA(1,2-B)PYRIDINE, 8-CHLORO-6,11-DIHYDRO-11-(1-((5-METHYL-3-PYRIDINYL)METHYL)-4-PIPERIDINYLIDENE)-, (2E)-2-BUTENEDIOATE (1:1)

Systematic Name

English

RUPATADINE FUMARATE [EP MONOGRAPH]

Common Name

English

Code System Code Type Description

DRUG BANK

DBSALT001922