Drug intelligence / Profile preview

lobeline

Development stage
Phase 2
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral, Inhalation, Transdermal, Intravenous
01

Overview

Lobeline is a piperidine alkaloid found in several plants of the Lobelia genus, including Indian tobacco (Lobelia inflata). It has been used historically as a smoking cessation aid and for respiratory disorders, though clinical evidence supporting its efficacy is limited. Lobeline acts primarily as a ligand at the vesicular monoamine transporter 2 (VMAT2), inhibiting dopamine uptake and promoting dopamine release from storage vesicles within presynaptic terminals. It also inhibits reuptake of dopamine and serotonin, functions as a mixed agonist–antagonist at nicotinic acetylcholine receptors (notably α3β2 and α4β2 subtypes), antagonizes μ-opioid receptors, and may inhibit P-glycoprotein. These mechanisms underlie its potential to modulate neurochemical pathways involved in addiction and neurodegenerative diseases such as Parkinson's disease. Despite preclinical promise for treating drug dependence (nicotine, amphetamines) and possible neuroprotective effects, there is little robust clinical evidence for approved therapeutic use[1][3][5][6][7][8].

Brand names
bantron
Other names
lobelinelobeline hydrochloride
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α3β2 nAChR (α3β2 nicotinic receptor)VMAT2 (Vesicular monoamine transporter 2)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

Beyond the preview

Go deeper on lobeline.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on lobeline.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call