Ligand id: 5281

Name: tranylcypromine

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View more information in the IUPHAR Pharmacology Education Project: tranylcypromine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 1
Hydrogen bond donors 1
Rotatable bonds 1
Topological polar surface area 26.02
Molecular weight 133.09
XLogP 3.18
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used in the treatment of major depressive episodes without melancholia.
The more recent observation that tranylcypromine inhibits the demethylase activity of lysine demethylase 1A (LSD1; KDM1A) has lead to its evaluation as an antinoplastic agent in acute myelogenous leukemia and myelodysplastic syndromes as an adjunct to chemotherapy with tretinoin. Development has reached Phase 1/2 for these conditions (see NCT02261779 as an example).
Mechanism Of Action and Pharmacodynamic Effects
Irreversible and non-selective monoamine oxidase inhibitor. Inhibition of monoamine oxidase leads to increased monoamine levels in the CNS, resulting in relief of depressive symptoms.
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