maprotiline
Trade name: ludiomil
Approved
Dec 1, 1980
Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TCAs in that it does not appear to block serotonin reuptake. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder (depressive neurosis) and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression. The mechanism of action of maprotiline is not precisely known. It does not act primarily by stimulation of the central nervous system and is not a monoamine oxidase inhibitor. The postulated mechanism of maprotiline is that it acts primarily by potentiation of central adrenergic synapses by blocking reuptake of norepinephrine at nerve endings. This pharmacologic action is thought to be responsible for the drug’s antidepressant and anxiolytic effects. The mean time to peak is 12 hours. The half-life of elimination averages 51 hours. — NCATS
Clinical trial activity
6 trials · 8 clinical orgs · 7 marketing orgs
Earliest trial started Jul 1, 2004 (NCT00183560)
Timeline
1980s
- Dec 1, 1980
Novartis — Earliest FDA Approval
- Dec 1, 1980
Novartis — NDA Secondary Org
- Dec 1, 1980
Novartis — NDA Organization
- Jun 1, 1988
Watson Pharmaceuticals — Marketing Organization
- Jun 1, 1988
Teva — Marketing Organization
- Jun 1, 1988
Heritage Pharma — Marketing Organization
- Oct 3, 1988
Rising Pharmaceuticals — Marketing Organization
- Oct 3, 1988
Mylan — Marketing Organization
2010s
- Jan 1, 2015
Earliest Phase 3 Sponsor(trial)
2020s
- Jan 1, 2020
Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Norepinephrine transporterINHIBITOR
SLC6A2 inhibitor
reuptake inhibitor
Approval history
- approvedDec 1, 1980
Chemistry & pharmacology
SMILES
CNCCCC12CCC(c3ccccc31)c1ccccc12- Mol. weight
- 277.41 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL21731 ↗
- WikipediaMaprotiline ↗
- NCATS2U1W68TROF ↗
- ChEMBLCHEMBL1237135 ↗
Also known as
- ba-34276 [as hydrochloride]
- ba-34276 [as hydrochloride]
- ludiomil
- ludiomil
- ludiomil
- maprotilina
- maprotilina
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline
- maprotiline hcl
- maprotiline hcl
- maprotiline hcl
- maprotiline hydrochloride
- maprotiline hydrochloride
- maprotiline hydrochloride
- maprotiline hydrochloride
- maprotilinum
- maprotilinum
- maprotylina
- maprotylina
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04200066 | Phase 1 | Feb 1, 2020 | University of Rochester |
| NCT02624102 | Phase 3 | Sep 1, 2015 | Federal University of Bahia, Hemanny, Curt, M.D. |
| NCT02374567 | Phase 3 | Jan 1, 2015 | Gottfried Wilhelm Leibniz Universität Hannover |
| NCT00158275 | N/A | Oct 1, 2004 | Group Health Cooperative, National Institute of Mental Health (NIMH) |
| NCT00118430 | Phase 4 | Sep 1, 2004 | Indiana University, National Institute of Mental Health (NIMH) |
| NCT00183560 | Phase 4 | Jul 1, 2004 | National Institute of Mental Health (NIMH), University of Toronto |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Institute of Mental Health (NIMH) | Government | 3 | 0 | 2 | 2004 |
| Federal University of Bahia | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Gottfried Wilhelm Leibniz Universität Hannover | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Group Health Cooperative | Academic/Hospital | 1 | 1 | 1 | 2004 |
| Hemanny, Curt, M.D. | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Indiana University | Academic/Hospital | 1 | 1 | 1 | 2004 |
| University of Rochester | Academic/Hospital | 1 | 1 | 1 | 2020 |
| University of Toronto | Academic/Hospital | 1 | 1 | 1 | 2004 |
Marketing (9)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Am Therap | For profit | MKTG | — |
| Heritage Pharma | For profit | MKTG | Jun 1, 1988 |
| Mylan | For profit | MKTG | Oct 3, 1988 |
| Novartis | For profit | NDA2 | Dec 1, 1980 |
| Novartis | For profit | NDA | Dec 1, 1980 |
| Rising Pharmaceuticals | For profit | MKTG | Oct 3, 1988 |
| Rising Pharmaceuticals | For profit | SYN | Oct 3, 1988 |
| Teva | For profit | MKTG | Jun 1, 1988 |
| Watson Pharmaceuticals | For profit | MKTG | Jun 1, 1988 |