isocarboxazid
Trade name: marplan
Approved
Jul 1, 1959
Isocarboxazid (Marplan, Marplon, Enerzer) is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class used as an antidepressant. In vivo and in vitro studies demonstrated inhibition of MAO in the brain, heart, and liver. Depression is a complicated disease that is not fully understood. It is thought that depression may be linked to an imbalance of chemicals within the brain. When depression occurs, there may be a decrease in the amount of chemicals released from nerve cells in the brain. These chemicals are called monoamines. Monoamines are broken down by a chemical called monoamine oxidase. Isocarboxazid prevents monoamine oxidase from breaking down the monoamines. This results in an increased amount of active monoamines in the brain. By increasing the amount of monoamines in the brain, the imbalance of chemicals thought to be caused by depression is altered. This helps relieve the symptoms of depression. Isocarboxazid works by irreversibly blocking the action of a chemical substance known as monoamine oxidase (MAO) in the nervous system. MAO subtypes A and B are involved in the metabolism of serotonin and catecholamine neurotransmitters such as epinephrine, norepinephrine, and dopamine. Isocarboxazid, as a nonselective MAO inhibitor, binds irreversibly to monoamine oxidase–A (MAO-A) and monoamine oxidase–B (MAO-B). The reduced MAO activity results in an increased concentration of these neurotransmitters in storage sites throughout the central nervous system (CNS) and sympathetic nervous system. This increased availability of one or more monoamines is the basis for the antidepressant activity of MAO inhibitors. May be used to treat major depressive disorder. — NCATS
Clinical trial activity
1 trials · 2 clinical orgs · 1 marketing orgs
Earliest trial started Jan 1, 2015 (NCT02323217)
Timeline
1950s
- Jul 1, 1959
Validus Pharmaceuticals — Earliest FDA Approval
- Jul 1, 1959
Validus Pharmaceuticals — NDA Secondary Org
- Jul 1, 1959
Validus Pharmaceuticals — NDA Organization
2010s
- Jan 1, 2015
Earliest Phase 1 Sponsor(trial)
Indications
Mechanism of action
- Monoamine oxidaseINHIBITOR
Monoamine oxidase inhibitor
Approval history
- approvedJul 1, 1959
Chemistry & pharmacology
SMILES
CC1=CC(=NO1)C(=O)NNCC2=CC=CC=C2- Mol. weight
- 231.2505 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
- WikipediaIsocarboxazid ↗
- NCATS34237V843T ↗
- ChEMBLCHEMBL2106317 ↗
- ChEMBLCHEMBL1201168 ↗
Also known as
- benazide
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazid
- isocarboxazida
- isocarboxazida
- isocarboxazide
- isocarboxazide
- isocarboxazide
- isocarboxazidum
- isocarboxazidum
- isocarboxyzid
- marplan
- marplan
- marplan
- marplan
- marplan
- marplan
- marplan
- ro 5-0831
- ro 5-0831/1
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02323217 | Early Phase 1 (Phase 1) | Jan 1, 2015 | GlaxoSmithKline, University of London |
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 1 | 0 | 1 | 2015 |
| University of London | Academic/Hospital | 1 | 1 | 1 | 2015 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Validus Pharmaceuticals | For profit | NDA2 | Jul 1, 1959 |
| Validus Pharmaceuticals | For profit | NDA | Jul 1, 1959 |