fexofenadine

Trade name: allegra

Small moleculeapproved

Approved

Jul 25, 1996

Fexofenadine is a second-generation, long lasting H1-receptor antagonist (antihistamine) which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Fexofenadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Fexofenadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Fexofenadine lacks the cardiotoxic potential of terfenadine, since it does not block the potassium channel involved in repolarization of cardiac cells. Fexofenadine is sold under the trade name Allegra among others. ALLEGRA is indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 2 years of age and older. — NCATS

Clinical trial activity

84 trials · 78 clinical orgs · 24 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jan 1, 2002 (NCT00835640)

Timeline

1990s

Jul 25, 1996
Sanofi-Aventis — Earliest FDA Approval
Jul 25, 1996
Sanofi-Aventis — NDA Secondary Org
Jul 25, 1996
Sanofi-Aventis — NDA Organization
Jul 25, 1996
Sanofi — NDA Secondary Org

2000s

Feb 25, 2000
Sanofi-Synthelabo — NDA Secondary Org
Jan 1, 2002
Teva — Earliest Phase 1 Sponsor(trial)
Jan 1, 2002
Sanofi — Earliest Phase 3 Sponsor(trial)
Apr 30, 2004
Mylan — Marketing Organization
Apr 14, 2005
Barr Laboratories — Marketing Organization
Sep 1, 2005
Teva — Marketing Organization
Jan 1, 2006
Earliest Phase 2 Sponsor(trial)
Apr 11, 2006
Dr. Reddy's Laboratories — Marketing Organization
Apr 16, 2007
Rising Pharmaceuticals — Marketing Organization
May 16, 2007
Ranbaxy — Marketing Organization
Apr 24, 2009
Sandoz — Marketing Organization
Apr 24, 2009
Novartis — Marketing Organization

2010s

Oct 19, 2010
Wockhardt — Marketing Organization
Nov 12, 2010
Impax Laboratories — Marketing Organization
Jul 25, 2012
Actavis — Marketing Organization
Jul 25, 2012
P&L Development — Marketing Organization
Jan 29, 2015
Sun Pharmaceuticals — Marketing Organization
Sep 16, 2015
Sciegen Pharmaceticals — Marketing Organization
Aug 19, 2016
Hetero Labs Ltd — Marketing Organization
Oct 30, 2017
Aurobindo Pharma — Marketing Organization
Nov 9, 2017
Taro Pharmaceuticals — Marketing Organization
Aug 13, 2018
Unique Pharmaceuticals Ltd, India — Marketing Organization
Oct 18, 2019
Granules India — Marketing Organization

2020s

Feb 24, 2020
Perrigo — Marketing Organization
Feb 28, 2025
Contract Pharmacal — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Histamine H1 receptorANTAGONIST
HRH1 antagonist
- Histamine H1 receptor (HRH1) ↗

Combination products

allegra-d 12 hour allergy and congestion
with pseudoephedrine
Also known as allegra-d 24 hour allergy and congestion, fexofenadine hcl; pseudoephedrine hcl

Approval history

approvedJul 25, 1996

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)(C(=O)O)c1ccc(C(O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1

Mol. weight: 501.67 g/mol
Lipinski Ro5: 2 violation(s)
Rule of 3: No
Chirality: Racemic Mixture
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Over the Counter

Oral

Yes

Parenteral

Topical

Sources

Also known as

4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid
4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid
4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid
allegra
allegra
allegra
allegra
allegra
allegra allergy
allegra allergy
allegra-d
allegra hives
allegra hives
alpha-(4-(1-carboxy-1-methylethyl)phenyl)-4-hydroxydiphenylmethyl-1-piperidinebutanol
aventis behring brand of fexofenadine hydrochloride
aventis brand of fexofenadine hydrochloride
aventis pharma brand of fexofenadine hydrochloride
carboxyterfenadine
carboxyterfenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine
fexofenadine hcl
fexofenadine hcl
fexofenadine hcl
fexofenadine hydrochloride
fexofenadine hydrochloride
fexofenadine hydrochloride
fexofenadine hydrochloride
fexofenadine hydrochloride
fexofenadine hydrochloride allergy
fexofenadine hydrochloride hives
hoechst brand of fexofenadine hydrochloride
mdl 16455
mdl 16.455
mdl-16455
mdl 16,455a
mdl-16455a
mdl-16455a
telfast
telfast 120
telfast 180
telfast 30
terfenadine acid metabolite
terfenadine acid metabolite
terfenadine carboxylate
terfenadine carboxylate
terfenadine carboxylate
terfenadine-cooh
terfenadine-cooh
terfenadine-cooh

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT07118215	Phase 1	Sep 29, 2025	Bristol-Myers Squibb, Karuna Pharmaceuticals
NCT06785298	Phase 2/Phase 3 (Phase 3)	Dec 10, 2024	Tanta University
NCT06548204	Phase 2	Sep 30, 2024	Zhejiang University
NCT05720455	Phase 4	Jul 21, 2024	Sanofi
NCT06466421	Phase 4	Jul 1, 2024	Helwan University, Tanta University
NCT06284902	Phase 1	Feb 23, 2024	Sanofi
NCT06205381	Phase 1	Jan 31, 2024	Aeovian Pharmaceuticals, Inc.
NCT06152497	N/A	Sep 1, 2023	Ghent University, Government of Belgium
NCT05932277	Phase 1	Jun 29, 2023	Bristol-Myers Squibb
NCT05692154	Phase 3	Jan 23, 2023	Sanofi
NCT05118672	Phase 3	Aug 17, 2022	Eurofarma Laboratorios S.A.
NCT05264025	Phase 1/Phase 2 (Phase 2)	Jun 1, 2022	October 6 University
NCT05461456	Phase 1	Apr 1, 2022	OrchestratePharma GmbH
NCT05263206	Phase 3	Feb 15, 2022	Sanofi
NCT04726345	Phase 2	Jun 29, 2021	Coloplast A/S, Columbia University, Queen's University, Belfast
NCT04688788	Phase 3	Jan 15, 2021	Aalborg University, Aarhus University, Central Jutland Regional Hospital, Danske Regioner, Hospital of Central Denmark Region, Viborg, Denmark, Hospital of South West Jutland, Region Syddanmark, University of Copenhagen, University of Southern Denmark
NCT04534153	Early Phase 1 (Phase 1)	Dec 31, 2020	Food and Drug Administration, University of California, San Francisco
NCT04224428	Phase 4	Jan 1, 2020	Tanta University
NCT04450134	N/A	Oct 2, 2019	Ghent University, Government of Belgium, University of Copenhagen
NCT03933007	Phase 4	May 1, 2019	Assistance Publique - Hôpitaux de Paris

Showing 20 of 84 trials

Page 1 / 5

Organizations

Research & Development (78)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Sanofi	For profit	21	21	3	2002
Dr. Reddy's Laboratories	For profit	5	5	1	2002
Merck	For profit	5	5	1	2002
Pfizer	For profit	3	3	2	2007
Tanta University	Academic/Hospital	3	3	2	2020
Bristol-Myers Squibb	For profit	2	1	1	2023
Eli Lilly	For profit	2	2	1	2016
Ghent University	Academic/Hospital	2	2	1	2019
GlaxoSmithKline	For profit	2	2	1	2006
Government of Belgium	Government	2	0	1	2019
Kendle International Inc.	For profit	2	0	1	2003
Mylan	For profit	2	2	1	2003
PRACS	For profit	2	0	1	2002
SFBC Anapharm	For profit	2	0	1	2002
Teva	For profit	2	2	1	2002
University of Copenhagen	Academic/Hospital	2	1	2	2019
Veeda Clinical Research	For profit	2	0	1	2007
Aalborg University	Academic/Hospital	1	0	1	2021
Aarhus University	Academic/Hospital	1	0	1	2021
Achillion Pharmaceuticals	For profit	1	1	1	2017

78 organizations

Page 1 / 4

Marketing (36)

Organization	Org type	Relationship	Date
Actavis	For profit	MKTG	Jul 25, 2012
Aurobindo Pharma	For profit	MKTG	Oct 30, 2017
Aurobindo Pharma	For profit	SYN	Nov 19, 2014
Aurobindo Pharma	For profit	SYN	Oct 30, 2017
Aurobindo Pharma	For profit	SYN	Nov 19, 2014
Barr Laboratories	For profit	MKTG	Apr 14, 2005
Contract Pharmacal	For profit	MKTG	Feb 28, 2025
Dr. Reddy's Laboratories	For profit	MKTG	Apr 11, 2006
Dr. Reddy's Laboratories	For profit	SYN	Nov 18, 2014
Granules India	For profit	SYN	Oct 18, 2019
Granules India	For profit	MKTG	Oct 18, 2019
Hetero Labs Ltd	For profit	MKTG	Aug 19, 2016
Impax Laboratories	For profit	MKTG	Nov 12, 2010
Mylan	For profit	MKTG	Apr 30, 2004
Novartis	For profit	MKTG	Apr 24, 2009
P&L Development	For profit	MKTG	Jul 25, 2012
Perrigo	For profit	MKTG	Feb 24, 2020
Perrigo	For profit	SYN	Feb 25, 2010
Ranbaxy	For profit	MKTG	May 16, 2007
Rising Pharmaceuticals	For profit	MKTG	Apr 16, 2007
Sandoz	For profit	MKTG	Apr 24, 2009
Sanofi	For profit	NDA2	Jul 25, 1996
Sanofi-Aventis	For profit	NDA2	Jul 25, 1996
Sanofi-Aventis	For profit	NDA	Jul 25, 1996
Sanofi-Synthelabo	For profit	NDA2	Feb 25, 2000
Sciegen Pharmaceticals	For profit	MKTG	Sep 16, 2015
Sun Pharmaceuticals	For profit	MKTG	Jan 29, 2015
Sun Pharmaceuticals	For profit	SYN	Feb 6, 2012
Sun Pharmaceuticals	For profit	SYN	Jan 29, 2015
Taro Pharmaceuticals	For profit	MKTG	Nov 9, 2017
Taro Pharmaceuticals	For profit	SYN	Nov 9, 2017
Teva	For profit	MKTG	Sep 1, 2005
Unique Pharmaceuticals Ltd, India	For profit	MKTG	Aug 13, 2018
Unique Pharmaceuticals Ltd, India	For profit	SYN	Aug 13, 2018
Wockhardt	For profit	MKTG	Oct 19, 2010
Wockhardt	For profit	SYN	Feb 8, 2012