selegiline

Trade name: zelapar

Small moleculeapprovedOrphan Drug FDA

Approved

Jun 5, 1989

Selegiline, also known as L-deprenyl, is a substituted phenethylamine, a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is available in pill form under many brand names (Eldepryl, Carbex, Atapryl) and is used to reduce symptoms in early-stage Parkinson's disease. Selegiline delays the time point when the L-DOPA (levodopa) treatment becomes necessary from about 11 months to about 18 months after diagnosis, which is beneficial despite not being definitive evidence of neuroprotection. The rationale for adding selegiline to levodopa is to decrease the required dose of levodopa and thus reduce the motor complications of levodopa therapy. Selegiline is also delivered via a transdermal patch (brand name, Emsam) and in this form, Selegiline is used as a treatment for the major depressive disorder. Selegiline (brand name Anipryl) is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and cognitive dysfunction (Canine Cognitive Dysfunction) in dogs. Side effects of the pill form include, in decreasing order of frequency, nausea, hallucinations, confusion, depression, loss of balance, insomnia, increased involuntary movements, agitation, arrhythmia, slow heart rate, delusions, hypertension, new or increased angina pectoris, and syncope. The main side effects of the patch form for depression included application site reactions, insomnia, diarrhea, and sore throat. — NCATS

Clinical trial activity

29 trials · 32 clinical orgs · 21 marketing orgs

Phase 1
4
Phase 2
14
Phase 3
3
Phase 4
8

Earliest trial started Sep 1, 1994 (NCT00000188)

Timeline

1980s

  1. Nov 7, 1984

    Orphan Drug Designation

  2. Jun 5, 1989

    Somerset Pharmaceuticals — Earliest FDA Approval

  3. Jun 5, 1989

    Somerset Pharmaceuticals — NDA Organization

  4. Jun 5, 1989

    Quagen Pharma — Marketing Organization

1990s

  1. Jan 1, 1994

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1994

    Earliest Phase 2 Sponsor(trial)

  3. Aug 2, 1996

    Chartwell Pharmaceuticals — Marketing Organization

  4. Aug 2, 1996

    G & W Laboratories Inc. — Marketing Organization

  5. Jan 27, 1997

    Cosette — Marketing Organization

  6. Jan 27, 1997

    ACP Nimble — Marketing Organization

  7. Apr 1, 1997

    Allied Pharmaceutical Services — Marketing Organization

  8. Apr 1, 1997

    Siegfried — Marketing Organization

  9. Apr 1, 1997

    I3 Pharms — Marketing Organization

  10. Jun 6, 1997

    Apotex — Marketing Organization

  11. Nov 26, 1997

    Mylan — Marketing Organization

  12. Nov 26, 1997

    Dash Pharms — Marketing Organization

  13. Apr 30, 1998

    Boscogen — Marketing Organization

  14. Apr 30, 1998

    Bayshore Pharms Llc — Marketing Organization

  15. Apr 30, 1998

    Kenton — Marketing Organization

  16. Nov 30, 1998

    DAVA Pharmaceuticals — Marketing Organization

  17. Nov 30, 1998

    Novitium Pharma — Marketing Organization

2000s

  1. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  2. Sep 15, 2003

    Lannett Company, Inc. — Marketing Organization

  3. Jun 14, 2006

    Bausch Health Companies — NDA Secondary Org

2010s

  1. Apr 2, 2019

    Pack Pharmaceuticals — Marketing Organization

  2. Apr 2, 2019

    Rising Pharmaceuticals — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewJun 5, 1989

Chemistry & pharmacology

Loading structure…

SMILES

C#CCN(C)[C@H](C)Cc1ccccc1
Mol. weight
187.29 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral, Topical
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

Yes

Black box warning

Sources

Also known as

  • anipryl
  • centrapryl 10
  • centrapryl 5
  • (-)-deprenil
  • (-)-deprenyl
  • eldepryl
  • eldepryl
  • eldepryl
  • emsam
  • emsam
  • ensam
  • ensam
  • l-deprenalin
  • l-deprenalin
  • l-deprenyl
  • l-deprenyl
  • l-deprenyl
  • (r)-(-)-deprenyl
  • (r)-selegiline
  • selegilina
  • selegilina
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • selegiline
  • (-)-selegiline
  • (−)-selegiline
  • (−)-selegiline
  • selegiline hcl
  • selegiline hcl
  • selegiline hcl
  • selegiline hydrochloride
  • selegiline hydrochloride
  • selegiline hydrochloride
  • selegiline hydrochloride
  • selegilinum
  • selegilinum
  • selegina
  • selgene
  • stilline 10
  • stilline 5
  • vivapryl
  • vivapryl
  • zelapar
  • zelapar
  • zelapar
  • zelapar

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05938517Phase 1Jun 2, 2021Ludwig Maximilians University
NCT04586543Phase 2May 18, 2020E-Group ICT Software Informatikai Zrt., University of Pecs
NCT04870372Phase 4Mar 1, 2020Soochow University
NCT04130087N/ASep 18, 2019University of Oxford
NCT02225548Phase 4Sep 1, 2014University of South Florida
NCT01912391Phase 3Oct 1, 2012Mood and Anxiety Research, Inc
NCT01495195Phase 2Feb 1, 2012Midwest Biomedical Research Foundation, National Institute on Drug Abuse (NIDA)
NCT00390923N/AJul 1, 2007Canadian Tobacco Control Research Initiative, University of Toronto
NCT00531947Phase 4Jul 1, 2007Cognitive Research Corporation, Somerset Pharmaceuticals
NCT00439413Phase 2Jun 1, 2007Department of Veteran Affairs, National Institute on Drug Abuse (NIDA)
NCT00531596Phase 4Apr 1, 2007Somerset Pharmaceuticals
NCT00456976Early Phase 1 (Phase 1)Apr 1, 2007University of Tabriz
NCT00532116Phase 4Apr 1, 2007Somerset Pharmaceuticals
NCT00443872Phase 4Mar 1, 2007Bausch Health Companies, Parkinson's Disease and Movement Disorder Center of Boca Raton, University of Kansas
NCT00535262Phase 4Mar 1, 2007Columbia University
NCT00640159Phase 4Jan 1, 2007Baylor University
NCT01330030Phase 2Jul 1, 2005National Institute on Drug Abuse (NIDA), Stanford University
NCT00218517Phase 2Mar 1, 2005National Institute on Drug Abuse (NIDA), Yale University
NCT00129311Phase 2Jul 1, 2004National Institute on Drug Abuse (NIDA), Yale University
NCT00285766Phase 3Aug 1, 2002Somerset Pharmaceuticals
Showing 20 of 29 trials
Page 1 / 2

Organizations

Research & Development (32)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Institute on Drug Abuse (NIDA)Government11731994
Somerset PharmaceuticalsFor profit5422001
Friends Research Institute, Inc.Academic/Hospital2021994
Johns Hopkins UniversityAcademic/Hospital2011999
National Institute of Allergy and Infectious Diseases (NIAID)Government2222001
Yale UniversityAcademic/Hospital2112004
Bausch Health CompaniesFor profit1012007
Baylor UniversityAcademic/Hospital1112007
Canadian Tobacco Control Research InitiativeAcademic/Hospital1012007
Cognitive Research CorporationFor profit1012007
Columbia UniversityAcademic/Hospital1112007
Department of Veteran AffairsGovernment1012007
E-Group ICT Software Informatikai Zrt.Academic/Hospital1012020
Icahn School of Medicine at Mount SinaiAcademic/Hospital1012001
Ludwig Maximilians UniversityAcademic/Hospital1112021
Midwest Biomedical Research FoundationAcademic/Hospital1112012
Mood and Anxiety Research, IncAcademic/Hospital1112012
National Institute of Neurological Disorders and Stroke (NINDS)Government1012001
Neurologic AIDS Research ConsortiumAcademic/Hospital1012001
Parkinson's Disease and Movement Disorder Center of Boca RatonAcademic/Hospital1112007
32 organizations
Page 1 / 2

Marketing (24)

OrganizationOrg typeRelationshipDate
ACP NimbleFor profitMKTGJan 27, 1997
Allied Pharmaceutical ServicesFor profitMKTGApr 1, 1997
ApotexFor profitSYNDec 4, 1998
ApotexFor profitMKTGJun 6, 1997
Bausch Health CompaniesFor profitNDA2Jun 14, 2006
Bausch Health CompaniesFor profitSYNJun 14, 2006
Bayshore Pharms LlcFor profitMKTGApr 30, 1998
BoscogenFor profitMKTGApr 30, 1998
Chartwell PharmaceuticalsFor profitMKTGAug 2, 1996
CosetteFor profitMKTGJan 27, 1997
DAVA PharmaceuticalsFor profitMKTGNov 30, 1998
Dash PharmsFor profitMKTGNov 26, 1997
G & W Laboratories Inc.For profitMKTGAug 2, 1996
I3 PharmsFor profitMKTGApr 1, 1997
KentonFor profitMKTGApr 30, 1998
Lannett Company, Inc.For profitMKTGSep 15, 2003
MylanFor profitSYNApr 1, 1997
MylanFor profitMKTGNov 26, 1997
Novitium PharmaFor profitMKTGNov 30, 1998
Pack PharmaceuticalsFor profitMKTGApr 2, 2019
Quagen PharmaFor profitMKTGJun 5, 1989
Rising PharmaceuticalsFor profitMKTGApr 2, 2019
SiegfriedFor profitMKTGApr 1, 1997
Somerset PharmaceuticalsFor profitNDAJun 5, 1989