cocaine
Trade name: Erythroxyline
Approved
Dec 14, 2017
Cocaine is an alkaloid ester extracted from the leaves of plants including coca. Cocaine is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death. Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar which can result in additional toxicity. Following repeated doses, a person may have decreased the ability to feel pleasure and be very physically tired. Cocaine acts by inhibiting the reuptake of serotonin, norepinephrine, and dopamine. This results in greater concentrations of these three neurotransmitters in the brain. It can easily cross the blood-brain barrier and may lead to the breakdown of the barrier. — NCATS
Clinical trial activity
52 trials · 29 clinical orgs · 5 marketing orgs
Earliest trial started May 1, 1995 (NCT00000270)
Timeline
1860s
- Jun 1, 1860
Evidence of US Marketing
1990s
- Jan 1, 1996
Earliest Phase 1 Sponsor(trial)
2000s
- Jan 1, 2005
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 1, 2014
Earliest Phase 3 Sponsor(trial)
- Dec 14, 2017
Earliest FDA Approval
- Dec 14, 2017
Noden Pharmaceuticals — Marketing Organization
- Dec 14, 2017
Genus Oncology, LLC — NDA Secondary Org
- Dec 19, 2017
Merck — First NDA Organization
- Dec 19, 2017
Merck — NDA Organization
2020s
- Jan 10, 2020
Cody Laboratories — Marketing Organization
- Jan 10, 2020
Cody Laboratories — NDA Secondary Org
- Jan 10, 2020
OMNIVIUM PHARMS — Marketing Organization
Indications
Approved for
Studied for
- Alcoholism · Phase 4
- Allergy and Immunology · Phase 1
- Analgesia · Phase 3
- Cocaine-Related Disorders · Phase 4
- Diagnosis · Phase 3
- Epistaxis · Phase 4
- Exercise · Phase 1/Phase 2
- General Surgery · Phase 3
- Healthy Volunteers · Phase 1
- Hyperthermia · Phase 1/Phase 2
- Nasal Obstruction · Phase 3
- Nose · Phase 3
- Opioid-Related Disorders · Phase 2
- Otolaryngology · Phase 4
- Pharmacokinetics · Phase 1
- Sinusitis · Phase 4
Mechanism of action
- Dopamine transporterANTAGONIST
SLC6A3 antagonist
- Sodium channel alpha subunitBLOCKER
Sodium channel alpha subunit blocker
Blocks voltage-gated sodium channels and prevents a rise in sodium conductance.
- Sodium channel protein type 1 subunit alpha (SCN1A) ↗
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗
- Sodium channel protein type 7 subunit alpha (SCN7A) ↗
- Sodium channel protein type 2 subunit alpha (SCN2A) ↗
- Sodium channel protein type 9 subunit alpha (SCN9A) ↗
- Sodium channel protein type 3 subunit alpha (SCN3A) ↗
- Sodium channel protein type 11 subunit alpha (SCN11A) ↗
- Sodium channel protein type 8 subunit alpha (SCN8A) ↗
- Sodium channel protein type 10 subunit alpha (SCN10A) ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type VII alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
Approval history
- approvedDec 14, 2017
- approvedJun 1, 1860
Chemistry & pharmacology
SMILES
COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C- Mol. weight
- 303.36 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL370805 ↗
- WikipediaCocaine ↗
- NCATSI5Y540LHVR ↗
- ChEMBLCHEMBL529437 ↗
Also known as
- [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid, methyl ester
- [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid, methyl ester
- 2-methyl-3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester)
- 2-methyl-3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester)
- cocain
- cocain
- cocain
- cocaina
- cocaina
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- cocaine
- (-)-cocaine
- (-)-cocaine
- (−)-cocaine
- (−)-cocaine
- cocaine hcl
- cocaine hcl
- cocaine hcl
- cocaine hydrochloride
- cocaine hydrochloride
- cocaine hydrochloride
- cocaine hydrochloride
- cocaine muriate
- cocainum
- cocainum
- kokain
- kokain
- l-cocain
- l-cocain
- l-cocaine
- l-cocaine
- methyl [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
- methyl [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
- methyl benzoylecgonine
- methyl benzoylecgonine
- neurocaine
- neurocaine
- rx0041
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07287735 | Phase 3 | Dec 6, 2025 | Omnivium Pharmaceuticals LLC |
| NCT07086794 | Early Phase 1 (Phase 1) | Nov 10, 2025 | National Institute on Drug Abuse (NIDA), University of Kentucky |
| NCT06443255 | Phase 3 | Jul 1, 2024 | University of Copenhagen |
| NCT06273540 | Phase 1 | Apr 15, 2024 | Altasciences Company Inc., National Institute on Drug Abuse (NIDA), Stalicla SA |
| NCT05809453 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2023 | The University of Texas, Dallas |
| NCT05334017 | Phase 4 | Sep 8, 2022 | University of Copenhagen |
| NCT05019430 | Early Phase 1 (Phase 1) | Oct 15, 2021 | National Institute on Drug Abuse (NIDA), University of Kentucky |
| NCT04792034 | Phase 4 | Apr 1, 2021 | Pharmaceutical Project Solutions, Inc. |
| NCT03937986 | Early Phase 1 (Phase 1) | Jul 1, 2019 | National Institute on Drug Abuse (NIDA), University of Kentucky |
| NCT03954938 | Early Phase 1 (Phase 1) | May 15, 2019 | University of Kentucky |
| NCT03519022 | Early Phase 1 (Phase 1) | Jun 1, 2018 | National Institute on Drug Abuse (NIDA), University of Kentucky |
| NCT03471182 | Phase 1 | Feb 26, 2018 | National Institute on Drug Abuse (NIDA), Yale University |
| NCT03018236 | Phase 4 | Jan 1, 2017 | Federal University of Rio Grande do Sul |
| NCT02856854 | Phase 1 | Jul 1, 2016 | Embera NeuroTherapeutics, Inc., National Institute on Drug Abuse (NIDA), Vince & Associates |
| NCT02775955 | Phase 1 | Feb 1, 2016 | Cognitive Research Corporation, Pharmaceutical Project Solutions, Inc. |
| NCT02775981 | Phase 1 | Feb 1, 2016 | Cognitive Research Corporation, Pharmaceutical Project Solutions, Inc. |
| NCT02563769 | Phase 1 | Feb 1, 2016 | National Institute on Drug Abuse (NIDA), Temple University, University of Pennsylvania |
| NCT02667106 | Phase 1 | Oct 1, 2015 | Pharmaceutical Project Solutions, Inc. |
| NCT02500836 | Phase 3 | Sep 1, 2015 | Lannett Company, Inc. |
| NCT02522325 | Phase 1 | Aug 1, 2015 | National Institute on Drug Abuse (NIDA), University of Kentucky |
Organizations
Research & Development (29)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Institute on Drug Abuse (NIDA) | Government | 26 | 8 | 4 | 1995 |
| University of Kentucky | Academic/Hospital | 11 | 11 | 1 | 2014 |
| Yale University | Academic/Hospital | 6 | 6 | 2 | 2012 |
| Columbia University | Academic/Hospital | 5 | 4 | 2 | 1995 |
| Pharmaceutical Project Solutions, Inc. | For profit | 5 | 5 | 3 | 2014 |
| The University of Texas, Dallas | Academic/Hospital | 4 | 2 | 2 | 2004 |
| Johns Hopkins University | Academic/Hospital | 3 | 1 | 2 | 1996 |
| Vince & Associates | For profit | 3 | 0 | 2 | 2013 |
| Cognitive Research Corporation | For profit | 2 | 0 | 1 | 2016 |
| Lannett Company, Inc. | For profit | 2 | 2 | 1 | 2014 |
| University of Copenhagen | Academic/Hospital | 2 | 2 | 2 | 2022 |
| Altasciences Company Inc. | For profit | 1 | 0 | 1 | 2024 |
| Baylor University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Biotie Therapies | For profit | 1 | 1 | 1 | 2008 |
| Brain & Behavior Research Foundation | Academic/Hospital | 1 | 0 | 1 | 2005 |
| Embera NeuroTherapeutics, Inc. | For profit | 1 | 1 | 1 | 2016 |
| Federal University of Rio Grande do Sul | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2005 |
| Indivior Inc. | For profit | 1 | 1 | 1 | 2013 |
| McGill University | Academic/Hospital | 1 | 1 | 1 | 2012 |
Marketing (6)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Cody Laboratories | For profit | MKTG | Jan 10, 2020 |
| Cody Laboratories | For profit | NDA2 | Jan 10, 2020 |
| Genus Oncology, LLC | For profit | NDA2 | Dec 14, 2017 |
| Merck | For profit | NDA | Dec 19, 2017 |
| Noden Pharmaceuticals | For profit | MKTG | Dec 14, 2017 |
| OMNIVIUM PHARMS | For profit | MKTG | Jan 10, 2020 |