cocaine

Trade name: Erythroxyline

Small moleculeapproved

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

Phase 1
33
Phase 2
13
Phase 3
5
Phase 4
5

Earliest trial started May 1, 1995 (NCT00000270)

Timeline

1860s

  1. Jun 1, 1860

    Evidence of US Marketing

1990s

  1. Jan 1, 1996

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2005

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2014

    Earliest Phase 3 Sponsor(trial)

  2. Dec 14, 2017

    Earliest FDA Approval

  3. Dec 14, 2017

    Noden Pharmaceuticals — Marketing Organization

  4. Dec 14, 2017

    Genus Oncology, LLC — NDA Secondary Org

  5. Dec 19, 2017

    Merck — First NDA Organization

  6. Dec 19, 2017

    Merck — NDA Organization

2020s

  1. Jan 10, 2020

    Cody Laboratories — Marketing Organization

  2. Jan 10, 2020

    Cody Laboratories — NDA Secondary Org

  3. Jan 10, 2020

    OMNIVIUM PHARMS — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedDec 14, 2017
  • approvedJun 1, 1860

Chemistry & pharmacology

Loading structure…

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

Black box warning

Sources

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 IDPhaseStart dateSponsor(s)
NCT07287735Phase 3Dec 6, 2025Omnivium Pharmaceuticals LLC
NCT07086794Early Phase 1 (Phase 1)Nov 10, 2025National Institute on Drug Abuse (NIDA), University of Kentucky
NCT06443255Phase 3Jul 1, 2024University of Copenhagen
NCT06273540Phase 1Apr 15, 2024Altasciences Company Inc., National Institute on Drug Abuse (NIDA), Stalicla SA
NCT05809453Phase 1/Phase 2 (Phase 2)Sep 1, 2023The University of Texas, Dallas
NCT05334017Phase 4Sep 8, 2022University of Copenhagen
NCT05019430Early Phase 1 (Phase 1)Oct 15, 2021National Institute on Drug Abuse (NIDA), University of Kentucky
NCT04792034Phase 4Apr 1, 2021Pharmaceutical Project Solutions, Inc.
NCT03937986Early Phase 1 (Phase 1)Jul 1, 2019National Institute on Drug Abuse (NIDA), University of Kentucky
NCT03954938Early Phase 1 (Phase 1)May 15, 2019University of Kentucky
NCT03519022Early Phase 1 (Phase 1)Jun 1, 2018National Institute on Drug Abuse (NIDA), University of Kentucky
NCT03471182Phase 1Feb 26, 2018National Institute on Drug Abuse (NIDA), Yale University
NCT03018236Phase 4Jan 1, 2017Federal University of Rio Grande do Sul
NCT02856854Phase 1Jul 1, 2016Embera NeuroTherapeutics, Inc., National Institute on Drug Abuse (NIDA), Vince & Associates
NCT02775955Phase 1Feb 1, 2016Cognitive Research Corporation, Pharmaceutical Project Solutions, Inc.
NCT02775981Phase 1Feb 1, 2016Cognitive Research Corporation, Pharmaceutical Project Solutions, Inc.
NCT02563769Phase 1Feb 1, 2016National Institute on Drug Abuse (NIDA), Temple University, University of Pennsylvania
NCT02667106Phase 1Oct 1, 2015Pharmaceutical Project Solutions, Inc.
NCT02500836Phase 3Sep 1, 2015Lannett Company, Inc.
NCT02522325Phase 1Aug 1, 2015National Institute on Drug Abuse (NIDA), University of Kentucky
Showing 20 of 52 trials
Page 1 / 3

Organizations

Research & Development (29)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute on Drug Abuse (NIDA)Government26841995
University of KentuckyAcademic/Hospital111112014
Yale UniversityAcademic/Hospital6622012
Columbia UniversityAcademic/Hospital5421995
Pharmaceutical Project Solutions, Inc.For profit5532014
The University of Texas, DallasAcademic/Hospital4222004
Johns Hopkins UniversityAcademic/Hospital3121996
Vince & AssociatesFor profit3022013
Cognitive Research CorporationFor profit2012016
Lannett Company, Inc.For profit2212014
University of CopenhagenAcademic/Hospital2222022
Altasciences Company Inc.For profit1012024
Baylor UniversityAcademic/Hospital1112015
Biotie TherapiesFor profit1112008
Brain & Behavior Research FoundationAcademic/Hospital1012005
Embera NeuroTherapeutics, Inc.For profit1112016
Federal University of Rio Grande do SulAcademic/Hospital1112017
Harvard UniversityAcademic/Hospital1012005
Indivior Inc.For profit1112013
McGill UniversityAcademic/Hospital1112012
29 organizations
Page 1 / 2

Marketing (6)

OrganizationOrg typeRelationshipDate
Cody LaboratoriesFor profitMKTGJan 10, 2020
Cody LaboratoriesFor profitNDA2Jan 10, 2020
Genus Oncology, LLCFor profitNDA2Dec 14, 2017
MerckFor profitNDADec 19, 2017
Noden PharmaceuticalsFor profitMKTGDec 14, 2017
OMNIVIUM PHARMSFor profitMKTGJan 10, 2020