benoxinate

Small moleculeapproved

Approved

Jan 14, 1975

Oxybuprocaine (benoxinate) hydrochloride (MINIMS®) is a local, surface anaesthetic of the ester type. It has been shown to give effective surface anaesthesia in short opthalmological procedures. Sensation of pain is locally and reversibly reduced, with the possibility of temperature and pressure sensitivity also affected. Anaesthetic activity is ten times that of cocaine and twice that of tetracaine (amethocaine). Oxybuprocaine (benoxinate) binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions. Depolarization of the neuronal membrane is inhibited thereby blocking the initiation and conduction of nerve impulses. — NCATS

Clinical trial activity

12 trials · 13 clinical orgs · 3 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jul 31, 2013 (NCT01901601)

Timeline

1970s

Jan 14, 1975
Johnson and Johnson — Earliest FDA Approval
Jan 14, 1975
Johnson and Johnson — NDA Organization
Jan 14, 1975
Johnson and Johnson — Marketing Organization

2010s

Dec 14, 2017
Altair Therapeutics — Marketing Organization
Dec 14, 2017
Altair Therapeutics — NDA Secondary Org
Jan 1, 2018
Earliest Phase 2 Sponsor(trial)

2020s

Jan 1, 2020
Earliest Phase 3 Sponsor(trial)
Mar 9, 2020
Bausch Health Companies — NDA Secondary Org
Jan 1, 2021
Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Pain (approved 2000)

Studied for

Mechanism of action

Sodium channel alpha subunitBLOCKER
Sodium channel alpha subunit blocker

Combination products

altafluor benox
with fluorescein

Approval history

approvedJan 14, 1975

Chemistry & pharmacology

Loading structure…

SMILES

CCCCOc1cc(C(=O)OCCN(CC)CC)ccc1N

Mol. weight: 308.42 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Topical
Availability: Prescription Only

Oral

Parenteral

Topical

Yes

Sources

Also known as

4-amino-3-butoxy-2-(diethylamino)ethyl ester benzoic acid
4-amino-3-butoxy-2-(diethylamino)ethyl ester benzoic acid
4-amino-3-butoxy-benzoic acid 2-diethylamino-ethyl ester
4-amino-3-butoxy-benzoic acid 2-diethylamino-ethyl ester
4-amino-3-n-butoxy-benzoesaeure-diaethylaminoaethylester
4-amino-3-n-butoxy-benzoesaeure-diaethylaminoaethylester
benoxil
benoxil
benoxinate
benoxinate
benoxinate
benoxinate
benoxinate
benoxinate
benoxinate
benoxinate
benoxinate dihydrochloride
benoxinate hcl
benoxinate hcl
benoxinate hcl
benoxinate hydrochloride
benoxinate hydrochloride
benoxinate hydrochloride
benoxinate hydrochloride
benoxinate hydrochloride
benoxinate monohydrochloride
bnx
bnx
butoxyaminobenzoyldiethylaminoethanol
butoxyaminobenzoyldiethylaminoethanol
butoxyprocaine
diethylaminoethyl-4-amino-3-butoxybenzoate
dorsecaine
novescine
novesin
oxibuprocaina
oxibuprocaina
oxibuprocaine chloride
oxibuprocaine chloride
oxybucaine
oxybucaine
oxybucaine
oxybuprocaine
oxybuprocaine
oxybuprocaine
oxybuprocaine
oxybuprocaine
oxybuprocaine
oxybuprocaine
oxybuprocaine hcl
oxybuprocaine hcl
oxybuprocainum
oxybuprocainum
oxyriprocaine
oxyriprocaine

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT05926258	Phase 3	Feb 29, 2024	Cross Research S.A., Sintetica SA
NCT05733741	Phase 4	Jan 30, 2023	Assiut University
NCT05666362	N/A	Mar 20, 2022	Alexandria University
NCT05069350	Early Phase 1 (Phase 1)	Sep 1, 2021	Research Institute of Ophthalmology, Egypt
NCT07230548	Phase 3	Jun 10, 2020	Medical University of Vienna
NCT04193774	N/A	Aug 19, 2019	Katholieke Universiteit Leuven
NCT03933280	Phase 2	Jun 30, 2019	Menoufia University
NCT03735368	Phase 2	Dec 10, 2018	Menoufia University
NCT04243811	N/A	Aug 15, 2018	Okan University
NCT02528123	N/A	Apr 1, 2016	London Vision Clinic
NCT01901614	N/A	Aug 31, 2013	National Eye Institute (NEI), National Institutes of Health (NIH), Oregon Health and Science University
NCT01901601	N/A	Jul 31, 2013	National Eye Institute (NEI), National Institutes of Health (NIH), Oregon Health and Science University

Showing 12 of 12 trials

Page 1 / 1

Organizations

Research & Development (13)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Menoufia University	Academic/Hospital	2	2	1	2018
National Eye Institute (NEI)	Government	2	0	1	2013
National Institutes of Health (NIH)	Government	2	0	1	2013
Oregon Health and Science University	Academic/Hospital	2	2	1	2013
Alexandria University	Academic/Hospital	1	1	1	2022
Assiut University	Academic/Hospital	1	1	1	2023
Cross Research S.A.	For profit	1	0	1	2024
Katholieke Universiteit Leuven	Academic/Hospital	1	1	1	2019
London Vision Clinic	Academic/Hospital	1	1	1	2016
Medical University of Vienna	Academic/Hospital	1	1	1	2020
Okan University	Academic/Hospital	1	1	1	2018
Research Institute of Ophthalmology, Egypt	Academic/Hospital	1	1	1	2021
Sintetica SA	For profit	1	1	1	2024

13 organizations

Page 1 / 1

Marketing (6)

Organization	Org type	Relationship	Date
Altair Therapeutics	For profit	MKTG	Dec 14, 2017
Altair Therapeutics	For profit	NDA2	Dec 14, 2017
Bausch Health Companies	For profit	NDA2	Mar 9, 2020
Bausch Health Companies	For profit	SYN	Mar 9, 2020
Johnson and Johnson	For profit	NDA	Jan 14, 1975
Johnson and Johnson	For profit	MKTG	Jan 14, 1975