benzonatate

Trade name: tessalon

Small moleculeapproved

Approved

Feb 10, 1958

Benzonatate is an antitussive that is FDA approved for the symptomatic relief of cough. It acts peripherally by anesthetizing the stretch receptors located in the respiratory passages, lungs, and pleura by dampening their activity and thereby reducing the cough reflex at its source. Common adverse reactions include nausea, oral hypoesthesia, throat symptom, numbness, dizziness, headache, sedation, somnolence. Benzonatate is chemically related to anesthetic agents of the para-amino-benzoic acid class (e.g. procaine; tetracaine) and has been associated with adverse CNS effects possibly related to a prior sensitivity to related agents or interaction with concomitant medication. — NCATS

Clinical trial activity

4 trials · 4 clinical orgs · 20 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jul 1, 2012 (NCT01690975)

Timeline

1950s

Feb 10, 1958
Ciba — Earliest FDA Approval
Feb 10, 1958
Pfizer — NDA Secondary Org
Feb 10, 1958
Ciba — NDA Organization

1990s

Jan 29, 1993
Bionpharma Inc — Marketing Organization

2000s

Mar 30, 2007
Thepharmanetwork Llc — Marketing Organization
Jun 8, 2007
Zydus Discovery DMCC — Marketing Organization
Jul 30, 2007
Alembic — Marketing Organization
Jul 30, 2007
Orit Labs Llc — Marketing Organization
Oct 31, 2007
Nesher Pharms — Marketing Organization
Mar 19, 2008
Sun Pharmaceuticals — Marketing Organization
Nov 9, 2009
Mikart — Marketing Organization

2010s

Jan 1, 2012
Pfizer — Earliest Phase 1 Sponsor(trial)
Jan 16, 2015
Acella Pharmaceuticals — Marketing Organization
Jan 16, 2015
Apotex — Marketing Organization
Jul 30, 2015
Strides Pharma Science — Marketing Organization
Jul 31, 2015
Shijiazhuang Pharma Group (CSPC) — Marketing Organization
Jan 1, 2018
Shijiazhuang Pharma Group (CSPC) — Earliest Phase 3 Sponsor(trial)
Nov 9, 2018
AiPing Pharm Inc — Marketing Organization
Nov 9, 2018
Baheal Pharmaceutical — Marketing Organization
Nov 9, 2018
Chartwell Pharmaceuticals — Marketing Organization
Dec 19, 2018
Puracap Pharmaceutical — Marketing Organization
Feb 22, 2019
Ascent Pharmahealth — Marketing Organization
Feb 22, 2019
Allergan PLC (2015) — Marketing Organization

Indications

Approved for

Cough

Studied for

Healthy Volunteers · Phase 1

Mechanism of action

Slowly adapting pulmonary stretch receptorINHIBITOR
Slowly adapting pulmonary stretch receptor inhibitor

Approval history

approvedFeb 10, 1958

Chemistry & pharmacology

Loading structure…

SMILES

CCCCNc1ccc(C(=O)OCCOCCOCCOCCOCCOCCOCCOCCOCCOC)cc1

Mol. weight: 603.75 g/mol
Lipinski Ro5: 2 violation(s)
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

Black box warning

Sources

Also known as

2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-butylaminobenzoate
2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-butylaminobenzoate
2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl p-(butylamino)benzoate
2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl p-(butylamino)benzoate
3,6,9,12,15,18,21,24,27-nonaoxaoctacosyl 4-butylaminobenzoate
3,6,9,12,15,18,21,24,27-nonaoxaoctacosyl 4-butylaminobenzoate
4-(butylamino)benzoic acid 3,6,9,12,15,18,21,24,27-nonaoxaoctacos-1-yl ester
4-(butylamino)benzoic acid 3,6,9,12,15,18,21,24,27-nonaoxaoctacos-1-yl ester
benzonatat
benzonatat
benzonatate
benzonatate
benzonatate
benzonatate
benzonatate
benzonatate
benzonatate
benzonatate
benzonatate
benzonatato
benzonatato
benzonatatum
benzonatatum
benzononantin
benzononatine
benzononatine
benzononatine
nonaethyleneglycol monomethyl ether p-n-butylaminobenzoate
nonaethyleneglycol monomethyl ether p-n-butylaminobenzoate
p-butylaminobenzoic acid omega-o-methylnonaethyleneglycol ester
p-butylaminobenzoic acid omega-o-methylnonaethyleneglycol ester
tessalon
tessalon
tessalon
tessalon
tessalon
tessalon
tessalon

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT03922373	Phase 1	Sep 10, 2018	Capital Medical University, Shijiazhuang Pharma Group (CSPC)
NCT03722914	Phase 3	Mar 1, 2018	Peking University, Shijiazhuang Pharma Group (CSPC)
NCT02207699	Phase 1	May 1, 2014	Pfizer
NCT01690975	Phase 1	Jul 1, 2012	Pfizer

Showing 4 of 4 trials

Page 1 / 1

Organizations

Research & Development (4)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Pfizer	For profit	2	2	1	2012
Shijiazhuang Pharma Group (CSPC)	For profit	2	2	2	2018
Capital Medical University	Academic/Hospital	1	0	1	2018
Peking University	Academic/Hospital	1	0	1	2018

4 organizations

Page 1 / 1

Marketing (22)

Organization	Org type	Relationship	Date
Acella Pharmaceuticals	For profit	MKTG	Jan 16, 2015
AiPing Pharm Inc	For profit	MKTG	Nov 9, 2018
Alembic	For profit	MKTG	Jul 30, 2007
Allergan PLC (2015)	For profit	MKTG	Feb 22, 2019
Apotex	For profit	MKTG	Jan 16, 2015
Ascent Pharmahealth	For profit	MKTG	Feb 22, 2019
Baheal Pharmaceutical	For profit	MKTG	Nov 9, 2018
Bionpharma Inc	For profit	MKTG	Jan 29, 1993
Bionpharma Inc	For profit	SYN	Jan 29, 1993
Chartwell Pharmaceuticals	For profit	MKTG	Nov 9, 2018
Ciba	For profit	NDA	Feb 10, 1958
Mikart	For profit	MKTG	Nov 9, 2009
Nesher Pharms	For profit	MKTG	Oct 31, 2007
Orit Labs Llc	For profit	MKTG	Jul 30, 2007
Pfizer	For profit	NDA2	Feb 10, 1958
Puracap Pharmaceutical	For profit	MKTG	Dec 19, 2018
Shijiazhuang Pharma Group (CSPC)	For profit	SYN	Jul 31, 2015
Shijiazhuang Pharma Group (CSPC)	For profit	MKTG	Jul 31, 2015
Strides Pharma Science	For profit	MKTG	Jul 30, 2015
Sun Pharmaceuticals	For profit	MKTG	Mar 19, 2008
Thepharmanetwork Llc	For profit	MKTG	Mar 30, 2007
Zydus Discovery DMCC	For profit	MKTG	Jun 8, 2007