CDEK by Data4ThePeople
Sign in Sign up
← All drugs Report issue

mefloquine

Trade name: lariam

Small moleculeapprovedOrphan Drug FDA

Approved

May 2, 1989

Mefloquine, sold under the brand names Lariam among others, is a medication used to for the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum. Mefloquine acts as a blood schizonticide. Mefloquine is active against the erythrocytic stages of Plasmodium species. However, the drug has no effect against the exoerythrocytic (hepatic) stages of the parasite. Mefloquine is effective against malaria parasites resistant to chloroquine. Mefloquine is a chiral molecule. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects. — NCATS

Clinical trial activity

54 trials · 94 clinical orgs · 8 marketing orgs

Phase 1
8
Phase 2
22
Phase 3
21
Phase 4
10

Earliest trial started Aug 1, 1998 (NCT02488902)

Timeline

1980s

  1. Apr 13, 1988

    Orphan Drug Designation

  2. May 2, 1989

    Roche — Earliest FDA Approval

  3. May 2, 1989

    United States Army — NDA Secondary Org

  4. May 2, 1989

    Roche — NDA Organization

1990s

  1. Jan 1, 1998

    United States Army — Earliest Phase 2 Sponsor(trial)

2000s

  1. Feb 20, 2002

    Sandoz — Marketing Organization

  2. Feb 20, 2002

    Novartis — Marketing Organization

  3. Feb 20, 2002

    Chartwell Pharmaceuticals — Marketing Organization

  4. Jan 1, 2003

    Earliest Phase 3 Sponsor(trial)

  5. Dec 29, 2003

    Barr Laboratories — Marketing Organization

  6. Oct 1, 2004

    West-Ward Pharmaceutical — Marketing Organization

  7. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Apr 21, 2010

    Hikma — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewMay 2, 1989

Chemistry & pharmacology

Loading structure…

SMILES

OC(c1cc(C(F)(F)F)nc2c(C(F)(F)F)cccc12)C1CCCCN1
Mol. weight
378.32 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
  • alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
  • benzenesulfonamide, 4-amino-n-(5,6-dimethoxy-4-pyrimidinyl)-, mixt. with 5-(4-chlorophenyl)-6-ethyl-2,4-pyrimidinediamine and (r*,s*)-(+-)-alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol monohydrochloride
  • fansimef
  • fansimef
  • fansimef
  • gnf-pf-5544
  • gnf-pf-5544
  • lariam
  • lariam
  • lariam
  • lariam
  • mefaquin
  • mefaquin
  • mefloquin
  • mefloquin
  • mefloquin
  • mefloquina
  • mefloquina
  • mefloquine
  • mefloquine
  • mefloquine
  • mefloquine
  • mefloquine
  • mefloquine
  • mefloquine
  • mefloquine
  • (+/-)-mefloquine
  • (+)-mefloquine
  • méfloquine
  • méfloquine
  • mefloquine hcl
  • mefloquine hcl
  • mefloquine hcl
  • mefloquine hydrochloride
  • mefloquine hydrochloride
  • mefloquine hydrochloride
  • mefloquine hydrochloride
  • mefloquine-sulfadoxine-pyrimethamine
  • mefloquinum
  • mefloquinum
  • mephaquin
  • mephloquine
  • mephloquine
  • mephloquine
  • mephloquine
  • mephloquine
  • mephloquine
  • mephloquine hcl
  • mephloquine hydrochloride
  • msp 4
  • ro-215998
  • ro-215998
  • ro-215998001
  • ro-215998001
  • [(r*,s*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
  • [(r*,s*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
  • wr-142490
  • wr-142490

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT04847661Phase 2/Phase 3 (Phase 3)Mar 28, 2021Ain Shams University, Assiut University, Fayoum University, Government of Japan, Helwan University, Tanta University
NCT04347031Phase 2Apr 8, 2020Burnasyan Federal Medical Biophysical Center
NCT03893097Phase 3Oct 14, 2019Institute of Tropical Medicine, Belgium
NCT03923725Phase 3Jul 1, 2019University of Oxford
NCT03939104Phase 3Jul 1, 2019University of Oxford
NCT03698695Phase 1Sep 27, 2018Theranexus, University of Lille
NCT03452475Phase 3Mar 10, 2018Mahidol University, University of Oxford
NCT01054248Phase 3Feb 1, 2016Mahidol University, University of Oxford
NCT02653898Phase 4Jan 1, 2016Government of Cambodia, Government of Thailand, National Center for Parasitology, Entomology and Malaria Control
NCT02612545Phase 1Nov 12, 2015National Institute of Allergy and Infectious Diseases (NIAID)
NCT02524444Phase 1Sep 1, 2015University of Ibadan
NCT02324738Phase 4Jan 1, 2015University of Oxford
NCT02084602Phase 4Jun 1, 2014Government of Peru, Instituto Nacional de Salud. Peru, United States Navy
NCT01640587N/ANov 1, 2013University of Oxford
NCT02052323Phase 4Oct 1, 2013Global Emerging Infections Surveillance and Response System, Government of Thailand, United States Army
NCT01976780Phase 4Jun 1, 2013Global Emerging Infections Surveillance and Response System, Kenya Medical Research Institute, United States Army
NCT01939886Phase 3Apr 1, 2013European Union, Kilimanjaro Christian Medical College, Tanzania, KIT Royal Tropical Institute, Radboud University, University of London
NCT02974348Phase 3Jan 1, 2013Chinese Academy of Medical Sciences, Government of China, University of Bamenda
NCT01708876Phase 3Oct 1, 2012Government of Malaysia, Menzies School of Health Research, Sabah Ministry of Health
NCT01615822Phase 1Aug 1, 2012Medicines for Malaria Venture, University of Cape Town
Showing 20 of 54 trials
Page 1 / 3

Organizations

Research & Development (94)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
University of OxfordAcademic/Hospital9832007
United States ArmyGovernment6331998
Centers for Disease Control and Prevention (CDC)Government5432005
Institute of Tropical Medicine, BelgiumAcademic/Hospital5522003
Mahidol UniversityAcademic/Hospital5032007
Medicines for Malaria VentureAcademic/Hospital4222007
University of LondonAcademic/Hospital4432005
Albert Schweitzer HospitalAcademic/Hospital3222005
Government of FranceGovernment3222005
Government of ThailandGovernment3322007
University of AntwerpAcademic/Hospital3022003
Centre MurazAcademic/Hospital2012008
Global Emerging Infections Surveillance and Response SystemGovernment2112013
Government of CambodiaGovernment2022007
Kenya Medical Research InstituteAcademic/Hospital2022009
Kilimanjaro Christian Medical College, TanzaniaAcademic/Hospital2012005
Kwame Nkrumah University of Science and TechnologyAcademic/Hospital2022007
Mepha Ltd.For profit2122005
National Institute for Medical Research, TanzaniaGovernment2012005
PfizerFor profit2212004
94 organizations
Page 1 / 5

Marketing (10)

OrganizationOrg typeRelationshipDate
Barr LaboratoriesFor profitMKTGDec 29, 2003
Chartwell PharmaceuticalsFor profitMKTGFeb 20, 2002
HikmaFor profitMKTGApr 21, 2010
HikmaFor profitSYNOct 1, 2004
HikmaFor profitSYNOct 1, 2004
NovartisFor profitMKTGFeb 20, 2002
RocheFor profitNDAMay 2, 1989
SandozFor profitMKTGFeb 20, 2002
United States ArmyGovernmentNDA2May 2, 1989
West-Ward PharmaceuticalFor profitMKTGOct 1, 2004